标签归档：mtor

PI3K/mTOR Inhibitor-6

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PI3K/mTOR Inhibitor-6 

PI3K/mTOR Inhibitor-6 (Compound 19c) 是一种有效的 PI3K/mTOR 双重抑制剂。PI3K/mTOR Inhibitor-6 在人工胃液中的稳定性优于 gedatolisib。PI3K/mTOR Inhibitor-6 在 10 μM 时显着抑制 PI3K/Akt/mTOR 信号通路。PI3K/mTOR Inhibitor-6具有研究癌症疾病的潜力。

PI3K/mTOR Inhibitor-6

PI3K/mTOR Inhibitor-6 Chemical Structure

CAS No. : 2456295-59-1

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

PI3K/mTOR Inhibitor-6 (Compound 19c) is a potent and dual inhibitor of PI3K/mTOR. PI3K/mTOR Inhibitor-6 displays better stability in artificial gastric fluids than gedatolisib. PI3K/mTOR Inhibitor-6 significantly suppresses the PI3K/Akt/mTOR signaling pathway at 10 μM. PI3K/mTOR Inhibitor-6 has the potential for the research of cancer diseases[1].

分子量

598.66

Formula

C30H34N10O4
CAS 号

2456295-59-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wang L, et al. Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors. Eur J Med Chem. 2020 Oct 15;204:112637

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PI3K/mTOR Inhibitor-7

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PI3K/mTOR Inhibitor-7 

PI3K/mTOR Inhibitor-7 (Compound 19i) 是一种有效的 PI3K/mTOR 双重抑制剂。PI3K/mTOR Inhibitor-7 的效力比阳性对照 gedatolisib 高 4.7 倍（0.3 对 1.4 μM，IC50 值）。PI3K/mTOR Inhibitor-7 在 10 μM 时显着抑制 PI3K/Akt/mTOR 信号通路。PI3K/mTOR Inhibitor-7 具有研究癌症疾病的潜力。

PI3K/mTOR Inhibitor-7

PI3K/mTOR Inhibitor-7 Chemical Structure

CAS No. : 2456295-65-9

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

PI3K/mTOR Inhibitor-7 (Compound 19i) is a potent and dual inhibitor of PI3K/mTOR. PI3K/mTOR Inhibitor-7 shows 4.7-fold higher potency than the positive control gedatolisib (0.3 vs. 1.4 μM, IC50 values). PI3K/mTOR Inhibitor-7 significantly suppresses the PI3K/Akt/mTOR signaling pathway at 10 μM. PI3K/mTOR Inhibitor-7 has the potential for the research of cancer diseases[1].

分子量

571.63

Formula

C29H33N9O4
CAS 号

2456295-65-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wang L, et al. Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors. Eur J Med Chem. 2020 Oct 15;204:112637

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

mTOR/HDAC6-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

mTOR/HDAC6-IN-1 

mTOR/HDAC6-IN-1 是一种有效的哺乳动物雷帕霉素 (mTOR) 和组蛋白去乙酰酶 (HDAC6) 的双重抑制剂 (mTOR 和 HDAC6 的 IC50s 分别为 133.7 nM 和 56 nM)。mTOR/HDAC6-IN-1 可诱导明显的细胞自噬 (autophagy)、细胞凋亡 (apoptosis)，以及抑制迁移。mTOR/HDAC6-IN-1 具有研究三阴性乳腺癌 (TNBC) 的潜力。

mTOR/HDAC6-IN-1

mTOR/HDAC6-IN-1 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

mTOR/HDAC6-IN-1 is a potent mTOR and HDAC6 dual inhibitor (IC50s of 133.7 nM and 56 nM for mTOR and HDAC6, respectively). mTOR/HDAC6-IN-1 can induce significant autophagy, apoptosis and suppress migration. mTOR/HDAC6-IN-1 has potential to research Triple-negative breast cancer (TNBC)[1].

IC50 & Target[1]

mTOR

133.7 nM (IC50)

HDAC6

56 nM (IC50)

体外研究
(In Vitro)

mTOR/HDAC6-IN-1 (compound 10g) (0-100 μM; 48 hours) has a medium anti-proliferation activity with IC50 of 8.4 μM, 10.6 μM and 14.3 μM in MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells at 48h[1].
mTOR/HDAC6-IN-1 (10 μM; 6 hours) can significantly improve the thermal stability of HDAC6 in MDA-MB-231 cells, which indicates that mTOR/HDAC6-IN-1 has a selective inhibitory effect on HDAC6[1].
mTOR/HDAC6-IN-1 (2.5, 5, 10 μM; 2 weeks) inhibits MDA-MB-231 cells form the clone[1].
mTOR/HDAC6-IN-1 (2.5, 5, 10 μM; 48 hours) induces obvious autophagy with the accumulation of LC3 puncta in MDA-MB-231 cells[1].
mTOR/HDAC6-IN-1 (5, 10, 20 μM) induces significant MDA-MB-231 apoptosis in a dose-dependent manner, also up-regulates the expression of Bax, down-regulates bcl-2, and promotes the cleavage of PARP and apoptotic executive protein caspase8 and caspase3[1].
mTOR/HDAC6-IN-1 (5, 10, 20 μM; 48 hours) inhibited MDA-MB-231 cells migration in a dose-dependent manner, and decreases the expression of MMP-2 as well as increases the expression of E-cadherin[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line: MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells[1]
Concentration: 0, 20, 40, 60, 80 and 100 μM
Incubation Time: 48 hours
Result: Had a medium anti-proliferation activity with IC50 of 8.4 μM, 10.6 μM and 14.3 μM in MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells at 48h.

Apoptosis Analysis

Cell Line: MDA-MB-231[1]
Concentration: 5, 10, 20 μM
Incubation Time:
Result: Induced significant MDA-MB-231 apoptosis in a dose-dependent manner, also up-regulates the expression of Bax, down-regulates bcl-2, and promotes the cleavage of PARP and apoptotic executive protein caspase8 and caspase3.

Cell Autophagy Assay

Cell Line: MDA-MB-231[1]
Concentration: 2.5, 5, 10 μM
Incubation Time: 48 hours
Result: Induced obvious autophagy with the accumulation of LC3 puncta in MDA-MB-231 cells

分子量

397.86

Formula

C20H20ClN5O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Yao D, et al. Design, synthesis and biological evaluation of dual mTOR/HDAC6 inhibitors in MDA-MB-231 cells. Bioorg Med Chem Lett. 2021;47:128204.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

mTOR/HDAC6-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

mTOR/HDAC6-IN-1 

mTOR/HDAC6-IN-1 是一种有效的哺乳动物雷帕霉素 (mTOR) 和组蛋白去乙酰酶 (HDAC6) 的双重抑制剂 (mTOR 和 HDAC6 的 IC50s 分别为 133.7 nM 和 56 nM)。mTOR/HDAC6-IN-1 可诱导明显的细胞自噬 (autophagy)、细胞凋亡 (apoptosis)，以及抑制迁移。mTOR/HDAC6-IN-1 具有研究三阴性乳腺癌 (TNBC) 的潜力。

mTOR/HDAC6-IN-1

mTOR/HDAC6-IN-1 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

mTOR/HDAC6-IN-1 is a potent mTOR and HDAC6 dual inhibitor (IC50s of 133.7 nM and 56 nM for mTOR and HDAC6, respectively). mTOR/HDAC6-IN-1 can induce significant autophagy, apoptosis and suppress migration. mTOR/HDAC6-IN-1 has potential to research Triple-negative breast cancer (TNBC)[1].

IC50 & Target[1]

mTOR

133.7 nM (IC50)

HDAC6

56 nM (IC50)

体外研究
(In Vitro)

mTOR/HDAC6-IN-1 (compound 10g) (0-100 μM; 48 hours) has a medium anti-proliferation activity with IC50 of 8.4 μM, 10.6 μM and 14.3 μM in MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells at 48h[1].
mTOR/HDAC6-IN-1 (10 μM; 6 hours) can significantly improve the thermal stability of HDAC6 in MDA-MB-231 cells, which indicates that mTOR/HDAC6-IN-1 has a selective inhibitory effect on HDAC6[1].
mTOR/HDAC6-IN-1 (2.5, 5, 10 μM; 2 weeks) inhibits MDA-MB-231 cells form the clone[1].
mTOR/HDAC6-IN-1 (2.5, 5, 10 μM; 48 hours) induces obvious autophagy with the accumulation of LC3 puncta in MDA-MB-231 cells[1].
mTOR/HDAC6-IN-1 (5, 10, 20 μM) induces significant MDA-MB-231 apoptosis in a dose-dependent manner, also up-regulates the expression of Bax, down-regulates bcl-2, and promotes the cleavage of PARP and apoptotic executive protein caspase8 and caspase3[1].
mTOR/HDAC6-IN-1 (5, 10, 20 μM; 48 hours) inhibited MDA-MB-231 cells migration in a dose-dependent manner, and decreases the expression of MMP-2 as well as increases the expression of E-cadherin[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line: MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells[1]
Concentration: 0, 20, 40, 60, 80 and 100 μM
Incubation Time: 48 hours
Result: Had a medium anti-proliferation activity with IC50 of 8.4 μM, 10.6 μM and 14.3 μM in MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells at 48h.

Apoptosis Analysis

Cell Line: MDA-MB-231[1]
Concentration: 5, 10, 20 μM
Incubation Time:
Result: Induced significant MDA-MB-231 apoptosis in a dose-dependent manner, also up-regulates the expression of Bax, down-regulates bcl-2, and promotes the cleavage of PARP and apoptotic executive protein caspase8 and caspase3.

Cell Autophagy Assay

Cell Line: MDA-MB-231[1]
Concentration: 2.5, 5, 10 μM
Incubation Time: 48 hours
Result: Induced obvious autophagy with the accumulation of LC3 puncta in MDA-MB-231 cells

分子量

397.86

Formula

C20H20ClN5O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Yao D, et al. Design, synthesis and biological evaluation of dual mTOR/HDAC6 inhibitors in MDA-MB-231 cells. Bioorg Med Chem Lett. 2021;47:128204.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

mTOR/HDAC6-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

mTOR/HDAC6-IN-1 

mTOR/HDAC6-IN-1 是一种有效的哺乳动物雷帕霉素 (mTOR) 和组蛋白去乙酰酶 (HDAC6) 的双重抑制剂 (mTOR 和 HDAC6 的 IC50s 分别为 133.7 nM 和 56 nM)。mTOR/HDAC6-IN-1 可诱导明显的细胞自噬 (autophagy)、细胞凋亡 (apoptosis)，以及抑制迁移。mTOR/HDAC6-IN-1 具有研究三阴性乳腺癌 (TNBC) 的潜力。

mTOR/HDAC6-IN-1

mTOR/HDAC6-IN-1 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

mTOR/HDAC6-IN-1 is a potent mTOR and HDAC6 dual inhibitor (IC50s of 133.7 nM and 56 nM for mTOR and HDAC6, respectively). mTOR/HDAC6-IN-1 can induce significant autophagy, apoptosis and suppress migration. mTOR/HDAC6-IN-1 has potential to research Triple-negative breast cancer (TNBC)[1].

IC50 & Target[1]

mTOR

133.7 nM (IC50)

HDAC6

56 nM (IC50)

体外研究
(In Vitro)

mTOR/HDAC6-IN-1 (compound 10g) (0-100 μM; 48 hours) has a medium anti-proliferation activity with IC50 of 8.4 μM, 10.6 μM and 14.3 μM in MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells at 48h[1].
mTOR/HDAC6-IN-1 (10 μM; 6 hours) can significantly improve the thermal stability of HDAC6 in MDA-MB-231 cells, which indicates that mTOR/HDAC6-IN-1 has a selective inhibitory effect on HDAC6[1].
mTOR/HDAC6-IN-1 (2.5, 5, 10 μM; 2 weeks) inhibits MDA-MB-231 cells form the clone[1].
mTOR/HDAC6-IN-1 (2.5, 5, 10 μM; 48 hours) induces obvious autophagy with the accumulation of LC3 puncta in MDA-MB-231 cells[1].
mTOR/HDAC6-IN-1 (5, 10, 20 μM) induces significant MDA-MB-231 apoptosis in a dose-dependent manner, also up-regulates the expression of Bax, down-regulates bcl-2, and promotes the cleavage of PARP and apoptotic executive protein caspase8 and caspase3[1].
mTOR/HDAC6-IN-1 (5, 10, 20 μM; 48 hours) inhibited MDA-MB-231 cells migration in a dose-dependent manner, and decreases the expression of MMP-2 as well as increases the expression of E-cadherin[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line: MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells[1]
Concentration: 0, 20, 40, 60, 80 and 100 μM
Incubation Time: 48 hours
Result: Had a medium anti-proliferation activity with IC50 of 8.4 μM, 10.6 μM and 14.3 μM in MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells at 48h.

Apoptosis Analysis

Cell Line: MDA-MB-231[1]
Concentration: 5, 10, 20 μM
Incubation Time:
Result: Induced significant MDA-MB-231 apoptosis in a dose-dependent manner, also up-regulates the expression of Bax, down-regulates bcl-2, and promotes the cleavage of PARP and apoptotic executive protein caspase8 and caspase3.

Cell Autophagy Assay

Cell Line: MDA-MB-231[1]
Concentration: 2.5, 5, 10 μM
Incubation Time: 48 hours
Result: Induced obvious autophagy with the accumulation of LC3 puncta in MDA-MB-231 cells

分子量

397.86

Formula

C20H20ClN5O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Yao D, et al. Design, synthesis and biological evaluation of dual mTOR/HDAC6 inhibitors in MDA-MB-231 cells. Bioorg Med Chem Lett. 2021;47:128204.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PI3K/Akt/mTOR-IN-2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PI3K/Akt/mTOR-IN-2 

PI3K/Akt/mTOR-IN-2 是一种有效的 PI3K/AKT/mTOR 抑制剂。PI3K/Akt/mTOR-IN-2 具有抗癌作用，并对 MDA-MB-231 细胞具有选择性，IC50 为 2.29 μM。PI3K/Akt/mTOR-IN-2 可诱导癌细胞周期阻滞和细胞凋亡 (apoptosis)。

PI3K/Akt/mTOR-IN-2

PI3K/Akt/mTOR-IN-2 Chemical Structure

CAS No. : 2757804-89-8

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

PI3K/Akt/mTOR-IN-2 is a PI3K/AKT/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-2 possess anti-cancer effects and selectivity against MDA-MB-231 cells with IC50 value of 2.29 μM. PI3K/Akt/mTOR-IN-2 can induce cancer cell cycle arrest and apoptosis[1].

IC50 & Target

IC50: 2.29 μM (PI3K/AKT/mTOR) in MDA-MB-231[1]
体外研究
(In Vitro)

PI3K/Akt/mTOR-IN-2 (compound 23) (0.5 – 100 μM; 72 hours) exhibits effective anti-cancer activity with IC50s of 2.29 – 24.63 μM, of which, IC50 in MDA-MB-231 is 2.29 μM[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24 hours) induces growth inhibition of MDA-MB-231 cells by cell cycle arrest at G0/G1[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24, 48 and 72 hours) induces apoptosis in MDA-MB-231 cells with both dose- and time-dependent manners[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 48 hours) increases the expression of Bax, and decreases the expression of Bcl-2 in MDA-MB-231 cells[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24 hours) induces mitochondria-dependent apoptosis in MDA-MB-231 cells through disruption of MMP, accumulation of ROS, depletion of GSH and elevation of intracellular Ca2+[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: PC3, BGC-823, A549, MCF-7, MDA-MB-231 cells and MCF-10A cells[1]
Concentration: 0.5 – 100 μM
Incubation Time: 72 hours
Result: Exhibited effective anti-cancer activity with IC50s of 2.29 – 24.63 μM, of which, IC50 in MDA-MB-231 was 2.29 μM.

Cell Cycle Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 24 hours
Result: Induced growth inhibition of MDA-MB-231 cells by cell cycle arrest at G0/G1.

Apoptosis Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 24, 48 and 72 hours
Result: Induced apoptosis in MDA-MB-231 cells with both dose- and time-dependent manners.

Western Blot Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 48 hours
Result: Increased the expression of Bax, and decreased the expression of Bcl-2

分子量

285.29

Formula

C17H13F2NO
CAS 号

2757804-89-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Qin J, Sun X, Ma Y, et al. Design, synthesis and biological evaluation of novel 1,3,4,9-tetrahydropyrano[3,4-b]indoles as potential treatment of triple negative breast cancer by suppressing PI3K/AKT/mTOR pathway [published online ahead of print, 2021 Dec 31]. Bioorg Med Chem. 2021;55:116594.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PI3K/Akt/mTOR-IN-2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PI3K/Akt/mTOR-IN-2 

PI3K/Akt/mTOR-IN-2 是一种有效的 PI3K/AKT/mTOR 抑制剂。PI3K/Akt/mTOR-IN-2 具有抗癌作用，并对 MDA-MB-231 细胞具有选择性，IC50 为 2.29 μM。PI3K/Akt/mTOR-IN-2 可诱导癌细胞周期阻滞和细胞凋亡 (apoptosis)。

PI3K/Akt/mTOR-IN-2

PI3K/Akt/mTOR-IN-2 Chemical Structure

CAS No. : 2757804-89-8

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

PI3K/Akt/mTOR-IN-2 is a PI3K/AKT/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-2 possess anti-cancer effects and selectivity against MDA-MB-231 cells with IC50 value of 2.29 μM. PI3K/Akt/mTOR-IN-2 can induce cancer cell cycle arrest and apoptosis[1].

IC50 & Target

IC50: 2.29 μM (PI3K/AKT/mTOR) in MDA-MB-231[1]
体外研究
(In Vitro)

PI3K/Akt/mTOR-IN-2 (compound 23) (0.5 – 100 μM; 72 hours) exhibits effective anti-cancer activity with IC50s of 2.29 – 24.63 μM, of which, IC50 in MDA-MB-231 is 2.29 μM[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24 hours) induces growth inhibition of MDA-MB-231 cells by cell cycle arrest at G0/G1[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24, 48 and 72 hours) induces apoptosis in MDA-MB-231 cells with both dose- and time-dependent manners[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 48 hours) increases the expression of Bax, and decreases the expression of Bcl-2 in MDA-MB-231 cells[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24 hours) induces mitochondria-dependent apoptosis in MDA-MB-231 cells through disruption of MMP, accumulation of ROS, depletion of GSH and elevation of intracellular Ca2+[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: PC3, BGC-823, A549, MCF-7, MDA-MB-231 cells and MCF-10A cells[1]
Concentration: 0.5 – 100 μM
Incubation Time: 72 hours
Result: Exhibited effective anti-cancer activity with IC50s of 2.29 – 24.63 μM, of which, IC50 in MDA-MB-231 was 2.29 μM.

Cell Cycle Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 24 hours
Result: Induced growth inhibition of MDA-MB-231 cells by cell cycle arrest at G0/G1.

Apoptosis Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 24, 48 and 72 hours
Result: Induced apoptosis in MDA-MB-231 cells with both dose- and time-dependent manners.

Western Blot Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 48 hours
Result: Increased the expression of Bax, and decreased the expression of Bcl-2

分子量

285.29

Formula

C17H13F2NO
CAS 号

2757804-89-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Qin J, Sun X, Ma Y, et al. Design, synthesis and biological evaluation of novel 1,3,4,9-tetrahydropyrano[3,4-b]indoles as potential treatment of triple negative breast cancer by suppressing PI3K/AKT/mTOR pathway [published online ahead of print, 2021 Dec 31]. Bioorg Med Chem. 2021;55:116594.

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PI3K/Akt/mTOR-IN-2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PI3K/Akt/mTOR-IN-2 

PI3K/Akt/mTOR-IN-2 是一种有效的 PI3K/AKT/mTOR 抑制剂。PI3K/Akt/mTOR-IN-2 具有抗癌作用，并对 MDA-MB-231 细胞具有选择性，IC50 为 2.29 μM。PI3K/Akt/mTOR-IN-2 可诱导癌细胞周期阻滞和细胞凋亡 (apoptosis)。

PI3K/Akt/mTOR-IN-2

PI3K/Akt/mTOR-IN-2 Chemical Structure

CAS No. : 2757804-89-8

规格 是否有货
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生物活性

PI3K/Akt/mTOR-IN-2 is a PI3K/AKT/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-2 possess anti-cancer effects and selectivity against MDA-MB-231 cells with IC50 value of 2.29 μM. PI3K/Akt/mTOR-IN-2 can induce cancer cell cycle arrest and apoptosis[1].

IC50 & Target

IC50: 2.29 μM (PI3K/AKT/mTOR) in MDA-MB-231[1]
体外研究
(In Vitro)

PI3K/Akt/mTOR-IN-2 (compound 23) (0.5 – 100 μM; 72 hours) exhibits effective anti-cancer activity with IC50s of 2.29 – 24.63 μM, of which, IC50 in MDA-MB-231 is 2.29 μM[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24 hours) induces growth inhibition of MDA-MB-231 cells by cell cycle arrest at G0/G1[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24, 48 and 72 hours) induces apoptosis in MDA-MB-231 cells with both dose- and time-dependent manners[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 48 hours) increases the expression of Bax, and decreases the expression of Bcl-2 in MDA-MB-231 cells[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24 hours) induces mitochondria-dependent apoptosis in MDA-MB-231 cells through disruption of MMP, accumulation of ROS, depletion of GSH and elevation of intracellular Ca2+[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: PC3, BGC-823, A549, MCF-7, MDA-MB-231 cells and MCF-10A cells[1]
Concentration: 0.5 – 100 μM
Incubation Time: 72 hours
Result: Exhibited effective anti-cancer activity with IC50s of 2.29 – 24.63 μM, of which, IC50 in MDA-MB-231 was 2.29 μM.

Cell Cycle Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 24 hours
Result: Induced growth inhibition of MDA-MB-231 cells by cell cycle arrest at G0/G1.

Apoptosis Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 24, 48 and 72 hours
Result: Induced apoptosis in MDA-MB-231 cells with both dose- and time-dependent manners.

Western Blot Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 48 hours
Result: Increased the expression of Bax, and decreased the expression of Bcl-2

分子量

285.29

Formula

C17H13F2NO
CAS 号

2757804-89-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Qin J, Sun X, Ma Y, et al. Design, synthesis and biological evaluation of novel 1,3,4,9-tetrahydropyrano[3,4-b]indoles as potential treatment of triple negative breast cancer by suppressing PI3K/AKT/mTOR pathway [published online ahead of print, 2021 Dec 31]. Bioorg Med Chem. 2021;55:116594.

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mTOR/HDAC-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

mTOR/HDAC-IN-1 

mTOR/HDAC-IN-1 (Compound 50) 是一个具有选择性的 mTOR 和 HDAC 双重抑制剂，对mTOR和HDAC1的 IC50 分别为0.49和0.91 nM。 mTOR/HDAC-IN-1 可作为抗癌药物 （anti-cancer） 进行研究。

mTOR/HDAC-IN-1

mTOR/HDAC-IN-1 Chemical Structure

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生物活性

mTOR/HDAC-IN-1 (Compound 50) is a selective mTOR and HDAC dual inhibitor with IC50 values of 0.49 and 0.91 nM against mTOR and HDAC1, respectively. mTOR/HDAC-IN-1 can be studied as an anti-cancer agent[1].

IC50 & Target

mTOR

0.49 nM (IC50)

HDAC1

0.91 nM (IC50)

HDAC6

86 nM (IC50)

HDAC8

27 nM (IC50)

体外研究
(In Vitro)

mTOR/HDAC-IN-1 (Compound 50) (0-10 μM, 72 h) shows remarkable anti-proliferative activity against A549, HCT116, and MV4-11 cells[1].
mTOR/HDAC-IN-1 (0-3 μM, 6 h) simultaneous modulates mTOR signaling and HDAC catalytic activity at cellular level[1].
mTOR/HDAC-IN-1 displays excellent specificity over both HDAC6 and HDAC11 (with IC50 values of 0.91, 86, 27, and >1000 against HDAC1, HDAC6, HDAC8 and HDAC11) [1].
mTOR/HDAC-IN-1 maintains the interaction of MLN0128 with the ATP-binding site in mTOR and binds with the catalytic channel in HDAC[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: A549, HCT116, and MV4-11
Concentration: 0-10 μM
Incubation Time: At 70 h post-compound treatment, to each well was added CCK-8, and the mixture was incubated for additional 2 h.
Result: Showed anti-proliferative activity with IC50 values of 2.16, 3.85, and 1.74 μM against A549, HCT116, and MV4-11 cells, respectively.

Western Blot Analysis[1]

Cell Line: MV4-11
Concentration: 0.3, 1.0, and 3.0 μM
Incubation Time: 6 h
Result: Downregulated the levels of Phos-S6 (Ser235/Ser236) and Phos-AKT (Ser473), and elevated the levels of Ac-H3 (K9) and Acα-tubulin (Lys40) in a concentration-dependent manner.

分子量

501.50

Formula

C23H23N11O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Mingming Zhang, et al. Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy. Bioorg Med Chem Lett. 2021 Oct 1;49:128286.

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mTOR/HDAC-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

mTOR/HDAC-IN-1 

mTOR/HDAC-IN-1 (Compound 50) 是一个具有选择性的 mTOR 和 HDAC 双重抑制剂，对mTOR和HDAC1的 IC50 分别为0.49和0.91 nM。 mTOR/HDAC-IN-1 可作为抗癌药物 （anti-cancer） 进行研究。

mTOR/HDAC-IN-1

mTOR/HDAC-IN-1 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

mTOR/HDAC-IN-1 (Compound 50) is a selective mTOR and HDAC dual inhibitor with IC50 values of 0.49 and 0.91 nM against mTOR and HDAC1, respectively. mTOR/HDAC-IN-1 can be studied as an anti-cancer agent[1].

IC50 & Target

mTOR

0.49 nM (IC50)

HDAC1

0.91 nM (IC50)

HDAC6

86 nM (IC50)

HDAC8

27 nM (IC50)

体外研究
(In Vitro)

mTOR/HDAC-IN-1 (Compound 50) (0-10 μM, 72 h) shows remarkable anti-proliferative activity against A549, HCT116, and MV4-11 cells[1].
mTOR/HDAC-IN-1 (0-3 μM, 6 h) simultaneous modulates mTOR signaling and HDAC catalytic activity at cellular level[1].
mTOR/HDAC-IN-1 displays excellent specificity over both HDAC6 and HDAC11 (with IC50 values of 0.91, 86, 27, and >1000 against HDAC1, HDAC6, HDAC8 and HDAC11) [1].
mTOR/HDAC-IN-1 maintains the interaction of MLN0128 with the ATP-binding site in mTOR and binds with the catalytic channel in HDAC[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: A549, HCT116, and MV4-11
Concentration: 0-10 μM
Incubation Time: At 70 h post-compound treatment, to each well was added CCK-8, and the mixture was incubated for additional 2 h.
Result: Showed anti-proliferative activity with IC50 values of 2.16, 3.85, and 1.74 μM against A549, HCT116, and MV4-11 cells, respectively.

Western Blot Analysis[1]

Cell Line: MV4-11
Concentration: 0.3, 1.0, and 3.0 μM
Incubation Time: 6 h
Result: Downregulated the levels of Phos-S6 (Ser235/Ser236) and Phos-AKT (Ser473), and elevated the levels of Ac-H3 (K9) and Acα-tubulin (Lys40) in a concentration-dependent manner.

分子量

501.50

Formula

C23H23N11O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Mingming Zhang, et al. Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy. Bioorg Med Chem Lett. 2021 Oct 1;49:128286.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

mTOR/HDAC-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

mTOR/HDAC-IN-1 

mTOR/HDAC-IN-1 (Compound 50) 是一个具有选择性的 mTOR 和 HDAC 双重抑制剂，对mTOR和HDAC1的 IC50 分别为0.49和0.91 nM。 mTOR/HDAC-IN-1 可作为抗癌药物 （anti-cancer） 进行研究。

mTOR/HDAC-IN-1

mTOR/HDAC-IN-1 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

mTOR/HDAC-IN-1 (Compound 50) is a selective mTOR and HDAC dual inhibitor with IC50 values of 0.49 and 0.91 nM against mTOR and HDAC1, respectively. mTOR/HDAC-IN-1 can be studied as an anti-cancer agent[1].

IC50 & Target

mTOR

0.49 nM (IC50)

HDAC1

0.91 nM (IC50)

HDAC6

86 nM (IC50)

HDAC8

27 nM (IC50)

体外研究
(In Vitro)

mTOR/HDAC-IN-1 (Compound 50) (0-10 μM, 72 h) shows remarkable anti-proliferative activity against A549, HCT116, and MV4-11 cells[1].
mTOR/HDAC-IN-1 (0-3 μM, 6 h) simultaneous modulates mTOR signaling and HDAC catalytic activity at cellular level[1].
mTOR/HDAC-IN-1 displays excellent specificity over both HDAC6 and HDAC11 (with IC50 values of 0.91, 86, 27, and >1000 against HDAC1, HDAC6, HDAC8 and HDAC11) [1].
mTOR/HDAC-IN-1 maintains the interaction of MLN0128 with the ATP-binding site in mTOR and binds with the catalytic channel in HDAC[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: A549, HCT116, and MV4-11
Concentration: 0-10 μM
Incubation Time: At 70 h post-compound treatment, to each well was added CCK-8, and the mixture was incubated for additional 2 h.
Result: Showed anti-proliferative activity with IC50 values of 2.16, 3.85, and 1.74 μM against A549, HCT116, and MV4-11 cells, respectively.

Western Blot Analysis[1]

Cell Line: MV4-11
Concentration: 0.3, 1.0, and 3.0 μM
Incubation Time: 6 h
Result: Downregulated the levels of Phos-S6 (Ser235/Ser236) and Phos-AKT (Ser473), and elevated the levels of Ac-H3 (K9) and Acα-tubulin (Lys40) in a concentration-dependent manner.

分子量

501.50

Formula

C23H23N11O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Mingming Zhang, et al. Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy. Bioorg Med Chem Lett. 2021 Oct 1;49:128286.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PI3K/mTOR Inhibitor-5

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PI3K/mTOR Inhibitor-5 

PI3K/mTOR Inhibitor-5 (compound 19a) 是一种有效的 PI3K 和 mTOR 双抑制剂，其 IC50 值分别为 86.9 nM 和 14.6 nM。

PI3K/mTOR Inhibitor-5

PI3K/mTOR Inhibitor-5 Chemical Structure

CAS No. : 2456295-60-4

规格 是否有货
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500 mg   询价  

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生物活性

PI3K/mTOR Inhibitor-5 (compound 19a) is a potent and dual PI3K and mTOR inhibitor, with IC50 values of 86.9 nM and 14.6 nM, respectively[1].

IC50 & Target

IC50: 86.9 nM (PI3K), 14.6 nM (mTOR)[1]
分子量

612.73

Formula

C32H40N10O3
CAS 号

2456295-60-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wu TT, Guo QQ, Chen ZL, et al. Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors. Eur J Med Chem. 2020;204:112637.

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PI3K/mTOR Inhibitor-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PI3K/mTOR Inhibitor-1 

PI3K/mTOR Inhibitor-1 是一种有效的，口服生物可利用的双重 PI3K/mTOR 抑制剂，抑制 PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ 和 mTOR，IC50 分别为 20/376/204/46 nM 和 186 nM。具有抗肿瘤活性。

PI3K/mTOR Inhibitor-1

PI3K/mTOR Inhibitor-1 Chemical Structure

CAS No. : 1949802-49-6

规格 是否有货
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250 mg   询价  
500 mg   询价  

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生物活性

PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively[1]. Antitumor activity[1].

IC50 & Target[1]

PI3Kα

20 nM (IC50)

PI3Kβ

376 nM (IC50)

PI3Kγ

204 nM (IC50)

PI3Kδ

46 nM (IC50)

mTOR

186 nM (IC50)

体外研究
(In Vitro)

PI3K/mTOR Inhibitor-1 (Compound 26) also exhibits potent functional suppression of AKT phosphorylation (IC50=196 nM)[1].
PI3K/mTOR Inhibitor-1 (0.046-10 µM, 72 hours) exhibits excellent antiproliferative effects on a panel of cancer cells. PI3K/mTOR Inhibitor inhibits A431, A549, PC3, MDA-MB-361, SW480, ES-2, HT29, SK-OV-3, HCT116 , G401 , BT20 ,DLD1 HCC827, H1650, H460, Farage, H820, HCT15, H358, Colo-205, PC9, H1975, WSU-DLCL2, HT, A2780, SU-DHL-10, Toledo,SU-DHL-6, DB, and Pfeiffer cells with IC50s of 0.188, 0.104, 0.063, 0.085, 0.534, 0.179, 0.163, 0.135, 0.308, 0.113, 0.729, 0.264, 0.287, 1.662, 0.611, 0.202, 0.365, 0.104, 0.098, 0.109, 0.237, 0.136, 0.145, 0.090, 0.251 0.215, 0.269, 0.111 0.062, and 0.061 µM, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: U87-MG, A431, MCF-7, PC3, A549, MDA-MB-361, SW480, ES-2, HT29, SK-OV-3, HCT116, G401, BT20, DLD1, HCC827, H1650, H460, Farage, H820, HCT15, H358, Colo-205, PC9, H1975, WSU-DLCL2, HT, A2780, SU-DHL-10, Toledo, SU-DHL-6, DB, Pfeiffer cells
Concentration: 0.046-10 µM
Incubation Time: 72 hours
Result: Inhibited HT-29 cells proliferation with an IC50 of 0.163 μM.

体内研究
(In Vivo)

PI3K/mTOR Inhibitor-1 (Compound 26) produces 54.4% tumor growth inhibition (TGI) with daily oral doses of 3.75 mg/kg for 27 days. The 7.5 mg/kg group of PI3K/mTOR Inhibitor-1 displays more significant TGI (72.9%). All animals survive after 27-day treatment, whereas 15% weigh loss is observed in PI3K/mTOR Inhibitor-1, 7.5 mg/kg group[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c nu/nu mice with HT-29 colorectal carcinoma xenograft mouse model carrying the PIK3CA P449T mutation[1]
Dosage: 3.75 and 7.5 mg/kg
Administration: Oral gavage daily for 27 days
Result: Tumor growth inhibition (TGI) was 54.4% and 72.9% for daily oral doses of 3.75 mg/kg and 7.5 mg/kg for 27 days, respectively.

分子量

407.46

Formula

C18H22FN5O3S
CAS 号

1949802-49-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Shen S, et al. Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines. ACS Med Chem Lett. 2018 Jun 25;9(7):719-724.

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mTOR inhibitor-2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

mTOR inhibitor-2 

mTOR inhibitor-2 是有效，选择性，可口服的 mTOR 抑制剂，IC50为7 nM。mTOR Inhibitor 1抑制mTORC1 (pS6 and p4E-BP1) 和mTORC2 (pAKT (S473)) 底物的细胞磷酸化。

mTOR inhibitor-2

mTOR inhibitor-2 Chemical Structure

CAS No. : 2219323-96-1

规格 是否有货
5 mg 询价
10 mg 询价
50 mg 询价
100 mg 询价

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生物活性

mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates[1].

IC50 & Target

mTOR

7 nM (IC50)

分子量

411.46

Formula

C23H21N7O
CAS 号

2219323-96-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Guo Q, et al. Highly Selective, Potent, and Oral mTOR Inhibitor for Treatment of Cancer as Autophagy Inducer. J Med Chem. 2018 Feb 8;61(3):881-904.

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MHY1485

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MHY1485  纯度: 99.86%

MHY1485 是一种有效的细胞渗透性 mTOR 激活剂，靶向 mTOR 的 ATP 结构域。MHY 1485 通过抑制自噬体和溶酶体之间的融合来抑制自噬 (autophagy)。

MHY1485

MHY1485 Chemical Structure

CAS No. : 326914-06-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥500 In-stock
5 mg ￥400 In-stock
10 mg ￥700 In-stock
50 mg ￥2500 In-stock
100 mg ￥4000 In-stock
200 mg ￥5800 In-stock
500 mg   询价  
1 g   询价  

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MHY1485 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Lipid Metabolism Compound Library
  • Glucose Metabolism Compound Library

生物活性

MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes[1].

IC50 & Target

mTORC1

 

mTORC2

 

Autophagy

 

体外研究
(In Vitro)

MHY1485 (10 μM; 4 hours) shows that GCDC-induced autophagic activity is inhibited by upregulating p-mTOR expression and downregulating LC3 and p62 expression in HCC cells[1].
MHY1485 (5 μM; 6 hours) increases the LC3II/LC3I ratio in a dose and time-dependently manner due to presumably inhibited LC3II degradation in rat liver Ac2F cells[2].
MHY1485 (0.5-2 μM; 6 hours) increases the phosphorylation of mTOR at ser2448 and upregulates the level of phosphorylation of 4E-BP1 in a dose-dependently manner in Ac2F cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HCC cells
Concentration: 10 μM
Incubation Time: 4 hours
Result: Upregulated p-mTOR and downregulated LC3 and p62 expression.

体内研究
(In Vivo)

MHY1485 (intraperitoneal injection; 10 mg/kg, 2 days) blocks the autophagy signaling induced by follicle-stimulating hormone (FSH). It increases p-mTOR and p-S6K1 expression levels, whereas LC3 expression shows no marked change compared to that in the control group[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4-week-old female ICR mice[3]
Dosage: 10 mg/kg, 2 days
Administration: Intraperitoneal injection
Result: Suppressed the autophagy level following FSH treatment. 

分子量

387.39

Formula

C17H21N7O4
CAS 号

326914-06-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 7.69 mg/mL (19.85 mM; Need ultrasonic)

H2O : 1 mg/mL (2.58 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5814 mL 12.9069 mL 25.8138 mL
5 mM 0.5163 mL 2.5814 mL 5.1628 mL
10 mM 0.2581 mL 1.2907 mL 2.5814 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.77 mg/mL (1.99 mM); Clear solution

    此方案可获得 ≥ 0.77 mg/mL (1.99 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 7.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 0.77 mg/mL (1.99 mM); Clear solution

    此方案可获得 ≥ 0.77 mg/mL (1.99 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 7.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Gao L, et al. Glycochenodeoxycholate promotes hepatocellular carcinoma invasion and migration by AMPK/mTOR dependent autophagy activation. Cancer Lett. 2019 Jul 10;454:215-223.

    [2]. Choi YJ, et al. Inhibitory effect of mTOR activator MHY1485 on autophagy: suppression of lysosomal fusion. PLoS One. 2012;7(8):e43418.

    [3]. Zhou J, et al.Administration of follicle-stimulating hormone induces autophagy via upregulation of HIF-1α in mouse granulosa cells.Cell Death Dis. 2017 Aug 17;8(8):e3001.

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mTOR inhibitor-3

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

mTOR inhibitor-3  纯度: 99.08%

mTOR inhibitor-3 是一种有效的 mTOR 抑制剂，Ki 值为 1.5 nM。mTOR inhibitor-3 在细胞实验及体内药代动力学 (PK)/药效学 (PD) 实验中都抑制 mTORC1 和 mTORC2。

mTOR inhibitor-3

mTOR inhibitor-3 Chemical Structure

CAS No. : 1207358-59-5

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥2088 In-stock
2 mg ￥1100 In-stock
5 mg ￥2000 In-stock
10 mg ￥2800 In-stock
50 mg ￥7500 In-stock
100 mg ￥13500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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•相关化合物库:

  • Covalent Screening Library Plus
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  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library
  • Antioxidants Compound Library
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  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Lipid Metabolism Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.

IC50 & Target[2]

mTOR

1.5 nM (Ki)

mTORC1

 

mTORC2

 

体外研究
(In Vitro)

mTOR inhibitor-3 (Compound 12i) inhibits mTOR with a Ki of 1.5 nM, 500-fold selectivity over closely related PI3 kinases. mTOR inhibitor-3 inhibits NCI-PC3 and MCF7neo/Her2 cells proliferation with IC50s of 150 nM and 57 nM, respectively[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

mTOR inhibitor-3 (Compound 8h) has high free plasma clearance in both mice (1818 mL/min/kg) and rats (1538 mL/min/kg in rat) [1]. mTOR inhibitor-3 (Compounds 12i) is selected for this study due to its potency, selectivity, and favorable mouse PK profile. Plasma levels of mTOR inhibitor-3 6 h following oral administration in PC3 tumor-bearing mice along with the fold decreases of phosphorylated mTORC1 and -2 substrates relative to time-matched vehicle controls. mTOR inhibitor-3 has moderate terminal elimination half-life (t1/2=1.7 h for mouse(1 mg/kg, iv)). mTOR inhibitor-3 achieves tumor stasis at the highest 200 mg/kg/day dose examined, which appears to also be approaching the limit of tolerability for this molecule[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

474.56

Formula

C25H30N8O2
CAS 号

1207358-59-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (105.36 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1072 mL 10.5361 mL 21.0722 mL
5 mM 0.4214 mL 2.1072 mL 4.2144 mL
10 mM 0.2107 mL 1.0536 mL 2.1072 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.27 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.27 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Pei Z, et al. Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349. ACS Med Chem Lett. 2012 Nov 29;4(1):103-7.

    [2]. Koehler MF, et al. Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity. J Med Chem. 2012 Dec 27;55(24):10958-71.
Animal Administration
[2]

Mice[2]
Human prostate cancer NCI-PC3 cells are implanted subcutaneously into the right hind flanks of female NCR nude mice (5×106 cells in 100 μL of Hank’s balanced salt solution). Tumors are monitored until they reach a mean tumor volume of approximately 500 mm3. Then similarly sized tumors are randomly assigned to groups (n=4). Compounds are formulated as suspensions in 0.5% methylcellulose/0.2% Tween 80 (MCT) and dosed orally at 25, 50, and 100 mg/kg (100 μL dose/25 g animal). Tumor and plasma samples are harvested at 1, 6, and 10 h postdose.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Pei Z, et al. Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349. ACS Med Chem Lett. 2012 Nov 29;4(1):103-7.

    [2]. Koehler MF, et al. Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity. J Med Chem. 2012 Dec 27;55(24):10958-71.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

HDACs/mTOR Inhibitor 1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

HDACs/mTOR Inhibitor 1  纯度: 98.21%

HDACs/mTOR Inhibitor 1 是组蛋白去乙酰酶抑制剂 (HDAC) 和哺乳动物雷帕霉素 (mTOR) 的双重抑制剂，有潜力用于恶性血液病的研究，其对 HDAC1、HDAC6、mTOR 和 PI3Kα 的 IC50 值分别为 0.19 nM、1.8 nM、1.2 nM 和 >500 nM。HDACs/mTOR Inhibitor 1 能够引起 G0/G1 期的细胞阻滞，诱导肿瘤细胞凋亡，在体内毒性较低。

HDACs/mTOR Inhibitor 1

HDACs/mTOR Inhibitor 1 Chemical Structure

CAS No. : 2271413-06-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5610 In-stock
5 mg ￥4500 In-stock
10 mg ￥7500 In-stock
50 mg ￥22500 In-stock
100 mg ￥33500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

HDACs/mTOR Inhibitor 1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Epigenetics Compound Library
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM and >500 nM for HDAC1, HDAC6, mTOR and PI3Kα, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induce tumor cell apoptosis with low toxicity in vivo[1].

IC50 & Target

HDAC1

0.19 nM (IC50)

HDAC6

1.8 nM (IC50)

mTOR

1.2 nM (IC50)

分子量

566.65

Formula

C28H38N8O5
CAS 号

2271413-06-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 32.5 mg/mL (57.35 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7648 mL 8.8238 mL 17.6476 mL
5 mM 0.3530 mL 1.7648 mL 3.5295 mL
10 mM 0.1765 mL 0.8824 mL 1.7648 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (3.83 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (3.83 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (3.83 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (3.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Chen Y, et al. Discovery of a Novel Dual Histone Deacetylases (HDACs) and Mammalian Target of Rapamycin (mTOR) Target Inhibitor as a Promising Strategy for Cancer Therapy. J Med Chem. 2019 Jan 10.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

RapaLink-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

RapaLink-1  纯度: 97.93%

RapaLink-1 是第三代 mTOR 抑制剂，通过 linker 将雷帕霉素 (Rapamycin, HY-10219) 与二代 mTOR 抑制剂 MLN0128 (HY-13328) 结合。RapaLink-1 比雷帕霉素或 mTOR 抑制剂 (TORKi) 更有效，能有效地阻断癌源性的，激活的 mTOR 突变体。RapaLink-1 可以穿过血脑屏障。RapaLink-1 与 FKBP12 的结合导致持久抑制 mTORC1。RapaLink-1 通过促进自噬在抗磷脂综合征中发挥抗血栓作用。具有抗癌活性。

RapaLink-1

RapaLink-1 Chemical Structure

CAS No. : 1887095-82-0

规格 价格 是否有货 数量
1 mg ￥4900 In-stock
5 mg ￥7000 In-stock
10 mg ￥12500 In-stock
25 mg ￥20000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

RapaLink-1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Macrocyclic Compound Library

生物活性

RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity[1][2].

IC50 & Target[1]

mTOR

 

体外研究
(In Vitro)

RapaLink-1 (0-200 nM; 3 days) shows U87MG cells growth inhibition[1].
RapaLink-1 (0-12.5 nM; 48 hours) arrests U87MG cells at G0/G1[1].
RapaLink-1 selectively inhibits p-RPS6S235/236 and p-4EBP1T37/46 at doses as low as 1.56 nM[1].
Rapalink-1 (100 nM; 24 to 96 hours) suppressed renal cell carcinoma (RCC) cell proliferation by inducing apoptosis and cell cycle arrest[2].
RapaLink-1 exploits the unique juxtaposition of two drug-binding pockets to create a bivalent interaction. RapaLink-1 overcomes resistance to existing first- and second-generation inhibitors[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: U87MG cells
Concentration: 0-200 nM
Incubation Time: 3 days
Result: Showed growth inhibition.

Cell Cycle Analysis[1]

Cell Line: U87MG cells
Concentration: 0-12.5 nM
Incubation Time: 48 hours
Result: Arrested cells at G0/G1.

Western Blot Analysis[1]

Cell Line: U87MG cells
Concentration: 0.39-12.5 nM
Incubation Time: 3 hours
Result: Selectively inhibited p-RPS6S235/236 and p-4EBP1T37/46 at doses as low as 1.56 nM. The mTORC2 targets p-AKTS473, p-SGK1S78, and p-NDRG1T346, and the p-AKTS473 target p-GSK3βS9 was inhibited only at high doses.

体内研究
(In Vivo)

RapaLink-1 (i.p.; every 5 days for 25 days, then once a week for 11 week) shows potent anti-tumor efficacy[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/ Cnu/nu mice bearing U87MG intracranial xenografts[1]
Dosage: 1.5 mg/kg
Administration: I.p.; every 5 days for 25 days, then once a week for 11 week
Result: Led to initial regression and subsequent stabilization of tumor size.

分子量

1784.14

Formula

C91H138N12O24
CAS 号

1887095-82-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 178 mg/mL (99.77 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.5605 mL 2.8025 mL 5.6049 mL
5 mM 0.1121 mL 0.5605 mL 1.1210 mL
10 mM 0.0560 mL 0.2802 mL 0.5605 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (2.80 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (2.80 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Fan Q, et al. A Kinase Inhibitor Targeted to mTORC1 Drives Regression in Glioblastoma. Cancer Cell. 2017 Mar 13;31(3):424-435.

    [2]. Kuroshima K, et al. Potential new therapy of Rapalink-1, a new generation mammalian target of rapamycin inhibitor, against SU 11248-resistant renal cell carcinoma. Cancer Sci. 2020 May;111(5):1607-1618.

    [3]. Rodrik-Outmezguine VS, et al. Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor. Nature. 2016 Jun 9;534(7606):272-6.

    [4]. Mu F, et al. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy both in vivo and vitro. Biochem Biophys Res Commun. 2020 Apr 30;525(2):384-391.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

mTOR inhibitor-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

mTOR inhibitor-1  纯度: 99.50%

mTOR inhibitor-1是新颖的 mTOR 通路抑制剂，可抑制细胞增殖，诱导自噬。

mTOR inhibitor-1

mTOR inhibitor-1 Chemical Structure

CAS No. : 468747-17-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2200 In-stock
5 mg ￥2000 In-stock
10 mg ￥4200 In-stock
50 mg ￥12000 In-stock
100 mg 询价

* Please select Quantity before adding items.

mTOR inhibitor-1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

mTOR inhibitor-1 is a novel mTOR pathway inhibitor which can suppress cells proliferation and inducing autophagy.

IC50 & Target

mTOR[1]
分子量

363.21

Formula

C16H15BrN2O3
CAS 号

468747-17-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL (229.43 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7532 mL 13.7661 mL 27.5323 mL
5 mM 0.5506 mL 2.7532 mL 5.5065 mL
10 mM 0.2753 mL 1.3766 mL 2.7532 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.73 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.73 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.73 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.73 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.73 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.73 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Liu J, et al. In Silico Discovery of a Small Molecule Suppressing Lung Carcinoma A549 Cells Proliferation and Inducing Autophagy via mTOR Pathway Inhibition. Mol Pharm. 2018 Nov 5;15(11):5427-5436.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

WAY-600

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

WAY-600  纯度: 95.12%

WAY-600 是有效，ATP 竞争型，选择性的 mTOR 抑制剂，抑制重组 mTOR 酶的 IC50 值为 9 nM。WAY-600 阻断 mTOR 复合物 1/2 (mTORC1/2) 组装和激活。

WAY-600

WAY-600 Chemical Structure

CAS No. : 1062159-35-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2067 In-stock
2 mg ￥1100 In-stock
5 mg ￥1900 In-stock
10 mg ￥2600 In-stock
50 mg ￥6900 In-stock
100 mg ￥11000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

WAY-600 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Lipid Metabolism Compound Library
  • Glucose Metabolism Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

WAY-600 is a potent, ATP-competitive, and selective mTOR inhibitor with an IC50 of 9 nM for recombinant mTOR enzyme. WAY-600 blocks mTOR complex 1/2 (mTORC1/2) assemble and activation.

IC50 & Target

mTOR

9 nM (IC50)

mTORC1

 

mTORC2

 

PI3K alpha

1.96 μM (IC50)

PI3K gamma

8.45 μM (IC50)

体外研究
(In Vitro)

WAY-600 exhibits a concentration-dependent and time-dependent inhibition of f HepG2 and Huh-7 cells viability. Following WAY-600 (1-1000 nM) treatment, the number of HepG2 cell colonies is dramatically decreased. Meanwhile, BrdU incorporation in HepG2 cells is also inhibited with WAY-600 treatment. WAY-600 dose-dependently increases the activity of caspase-3 and caspase-9 in HepG2 cells. WAY-600 disrupts assemble of mTORC1 (mTOR-Raptor association) and mTORC2 (mTOR-Rictor association). Activation of mTORC1 (indicated by p-S6K1 and p-4E-BP1) and mTORC2 is almost blocked by WAY-600 (100 nM)[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Administration of WAY-600 (10 mg/kg, daily) inhibits HepG2 tumor growth in nude mice. Daily HepG2 tumor growth of WAY-600-administrated mice is significantly lower than that of vehicle control mice. Importantly, the in vivo anti-cancer activity by WAY-600 is further potentiated with the co-administration of MEK-162 (2.5 mg/kg, p.o. daily)[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

494.59

Formula

C28H30N8O
CAS 号

1062159-35-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (101.09 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0219 mL 10.1094 mL 20.2188 mL
5 mM 0.4044 mL 2.0219 mL 4.0438 mL
10 mM 0.2022 mL 1.0109 mL 2.0219 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.05 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.05 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Yu K, et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res. 2009 Aug 1;69(15):6232-40.

    [2]. Wang K, et al. MEK-ERK inhibition potentiates WAY-600-induced anti-cancer efficiency in preclinical hepatocellular carcinoma (HCC) models. Biochem Biophys Res Commun. 2016 May 27;474(2):330-7.
Cell Assay
[2]

Established HCC cells (HepG2 and Huh-7), primary HCC cells (Pnt-1/-2/-3/-4), or THLE-2 liver cells are cultured in WAY-600 (1-1000 nM)-containing medium for 24, 48, 72, 96 hours, cell viability is tested by MTT assay[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice: Mice tumor xenografts are randomly divided into four groups (10 mice per group): vehicle ( intraperitoneal or i.p.), WAY-600 (10 mg/kg, i.p. injection), MEK-162 (2.5 mg/kg, oral gavage) or WAY-600 plus MEK-162 combination. The mice are monitored for activity and physical condition on daily basis, and mice body weights and tumor mass are measured weekly[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Yu K, et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res. 2009 Aug 1;69(15):6232-40.

    [2]. Wang K, et al. MEK-ERK inhibition potentiates WAY-600-induced anti-cancer efficiency in preclinical hepatocellular carcinoma (HCC) models. Biochem Biophys Res Commun. 2016 May 27;474(2):330-7.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务