标签归档：ros

Taletrectinib(Synonyms: DS-6051b; AB-106)

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。

Taletrectinib (Synonyms: DS-6051b; AB-106) 纯度: 99.96%

Taletrectinib (DS-6051b) 是一种有效的口服活性下一代选择性 ROS1/NTRK 抑制剂。Taletrectinib 分别以 0.207、0.622、2.28 和 0.98 nM 的 IC50 对重组 ROS1、NTRK1、NTRK2 和 NTRK3 有较强的抑制作用。Taletrectinib 还抑制 ROS1 G2032R 和其他抗 Crizotinib 的 ROS1 突变体。

Taletrectinib(Synonyms: DS-6051b; AB-106)

Taletrectinib Chemical Structure

CAS No. : 1505515-69-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3400 In-stock
5 mg ￥2800 In-stock
10 mg ￥4800 In-stock
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

Taletrectinib 相关产品

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生物活性

Taletrectinib (DS-6051b) is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants[1][2].

体外研究
(In Vitro)

The IC50 of Taletrectinib (1-1000 nM; 72 hours) against Ba/F3-TPM3-NTRK1, Ba/F3-ETV6-NTRK1, -NTRK2, -NTRK3, or KM12 cells is ~3-20 nM[1].
Taletrectinib (0.001-1000 nM; 2 hours) dose dependently inhibited autophosphorylation of ROS1 in U-118-MG cells in vitro[1].
Taletrectinib potently inhibits autophosphorylation of ROS1 in JFCR-165, JFCR-168, and MGH193-1B cells[1].
Taletrectinib partially suppresses phospho-NTRK1 at 10 nM, and completely suppresses by 100 nM. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, and NTRK3 in sub-nanomolar concentration in an ATP-competitive manner. Taletrectinib almost completely inhibits ACK, ALK, DDR1, and LTK at 0.2 μM among 160 kinases in the presence of 1 mM ATP, but did not inhibit other 152 kinases strongly[1].
Taletrectinib effectively inhibits Crizotinib-resistant ROS1 secondary mutations, including G2032R solvent front mutation[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[1]

Cell Line: TPM3-NTRK1-induced Ba/F3 cells, KM12 cells
Concentration: 1-1000 nM
Incubation Time: 72 hours
Result: Inhibited TPM3-NTRK1-induced Ba/F3 cells and KM12 cells viability.

Western Blot Analysis[1]

Cell Line: U-118 MG cells (harboring FIG-ROS1 fusion gene)
Concentration: 0.001-1000 nM
Incubation Time: 2 hours
Result: Dose dependently inhibited autophosphorylation of ROS1 in U-118-MG cells.

体内研究
(In Vivo)

Taletrectinib (DS-6051b) (25-200 mg/kg; p.o.; once daily for 18 days) shows antitumor activity[1].
Taletrectinib (6.25-200 mg/kg; p.o.; once daily for 8 days) inhibits NTRK-rearranged cancer in Balb-c nu/nu mice bearing KM12 cells[1].
Taletrectinib (3-100 mg/kg; p.o.; once daily for 4 days) shows rapid tumor regression in the wild-type (WT) and the G2032R-mutant Ba/F3-bearing mice without severe body weight loss[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 (bearing U-118 MG cells)[1]
Dosage: 25, 50, 100, and 200 mg/kg
Administration: P.o.; once daily for 18 days
Result: Effectively inhibited tumor growth at ≥25 mg/kg without significant body weight loss.

Clinical Trial

分子量

551.61

Formula

C29H34FN5O5
CAS 号

1505515-69-4
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 : 50 mg/mL (90.64 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8129 mL 9.0644 mL 18.1287 mL
5 mM 0.3626 mL 1.8129 mL 3.6258 mL
10 mM 0.1813 mL 0.9064 mL 1.8129 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    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.77 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.77 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 (3.77 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.77 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 (3.77 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.77 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]. Katayama R, et al. The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models. Nat Commun. 2019;10(1):3604. Published 2019 Aug 9.

    [2]. Fujiwara Y, et al. Safety and pharmacokinetics of DS-6051b in Japanese patients with non-small cell lung cancer harboring ROS1 fusions: a phase I study. Oncotarget. 2018;9(34):23729-23737. Published 2018 May 4.

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ALK/ROS1-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。

ALK/ROS1-IN-1 

ALK/ROS1-IN-1 (compound 2e) 是一种高效、选择性的抗 crizotinib 耐受 ALK/ROS1 双重抑制剂，对 ALK 和 ROS1 酶作用的 IC50 值分别为 0.174 μM 和 0.530 μM。

ALK/ROS1-IN-1

ALK/ROS1-IN-1 Chemical Structure

CAS No. : 2365497-07-8

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

ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.

IC50 & Target

IC50: 0.174 μM (ALK), 0.530 μM (ROS1)[1]
体外研究
(In Vitro)

ALK/ROS1-IN-1 displays potent anti-proliferative activity against ALK-addicted H3122 and ROS1-addicted HCC78 cell lines (IC50= 6.27 μM and 10.71 μM, respectively)[1].
ALK/ROS1-IN-1 shows impressive enzyme activity against clinically Crizotinib-resistant ALKL1196M with an IC50 value of 41.3 nM[1].
ALK/ROS1-IN-1 shows potent inhibitory activity in Ba/F3 cell line expressing ROS1 mutants, with IC50s of 137.7, 104.7 nM and 233.9 for wide-type, G2032R mutant and L2026M mutant, respectively[1].
ALK/ROS1-IN-1 has no significant effect on inducing apoptosis of HCC78 cell line[1].

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

584.63

Formula

C30H35F3N6O3
CAS 号

2365497-07-8
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]. Liu S, et al. Design, synthesis and biological evaluations of 2-amino-4-(1-piperidine) pyridine derivatives as novel anti crizotinib-resistant ALK/ROS1 dual inhibitors. Eur J Med Chem. 2019 Oct 1;179:358-375.

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

ALK/ROS1-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。

ALK/ROS1-IN-1 

ALK/ROS1-IN-1 (compound 2e) 是一种高效、选择性的抗 crizotinib 耐受 ALK/ROS1 双重抑制剂，对 ALK 和 ROS1 酶作用的 IC50 值分别为 0.174 μM 和 0.530 μM。

ALK/ROS1-IN-1

ALK/ROS1-IN-1 Chemical Structure

CAS No. : 2365497-07-8

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

ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.

IC50 & Target

IC50: 0.174 μM (ALK), 0.530 μM (ROS1)[1]
体外研究
(In Vitro)

ALK/ROS1-IN-1 displays potent anti-proliferative activity against ALK-addicted H3122 and ROS1-addicted HCC78 cell lines (IC50= 6.27 μM and 10.71 μM, respectively)[1].
ALK/ROS1-IN-1 shows impressive enzyme activity against clinically Crizotinib-resistant ALKL1196M with an IC50 value of 41.3 nM[1].
ALK/ROS1-IN-1 shows potent inhibitory activity in Ba/F3 cell line expressing ROS1 mutants, with IC50s of 137.7, 104.7 nM and 233.9 for wide-type, G2032R mutant and L2026M mutant, respectively[1].
ALK/ROS1-IN-1 has no significant effect on inducing apoptosis of HCC78 cell line[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.
分子量

584.63

Formula

C30H35F3N6O3
CAS 号

2365497-07-8
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]. Liu S, et al. Design, synthesis and biological evaluations of 2-amino-4-(1-piperidine) pyridine derivatives as novel anti crizotinib-resistant ALK/ROS1 dual inhibitors. Eur J Med Chem. 2019 Oct 1;179:358-375.

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

ALK/ROS1-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。

ALK/ROS1-IN-1 

ALK/ROS1-IN-1 (compound 2e) 是一种高效、选择性的抗 crizotinib 耐受 ALK/ROS1 双重抑制剂，对 ALK 和 ROS1 酶作用的 IC50 值分别为 0.174 μM 和 0.530 μM。

ALK/ROS1-IN-1

ALK/ROS1-IN-1 Chemical Structure

CAS No. : 2365497-07-8

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

ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.

IC50 & Target

IC50: 0.174 μM (ALK), 0.530 μM (ROS1)[1]
体外研究
(In Vitro)

ALK/ROS1-IN-1 displays potent anti-proliferative activity against ALK-addicted H3122 and ROS1-addicted HCC78 cell lines (IC50= 6.27 μM and 10.71 μM, respectively)[1].
ALK/ROS1-IN-1 shows impressive enzyme activity against clinically Crizotinib-resistant ALKL1196M with an IC50 value of 41.3 nM[1].
ALK/ROS1-IN-1 shows potent inhibitory activity in Ba/F3 cell line expressing ROS1 mutants, with IC50s of 137.7, 104.7 nM and 233.9 for wide-type, G2032R mutant and L2026M mutant, respectively[1].
ALK/ROS1-IN-1 has no significant effect on inducing apoptosis of HCC78 cell line[1].

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

584.63

Formula

C30H35F3N6O3
CAS 号

2365497-07-8
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]. Liu S, et al. Design, synthesis and biological evaluations of 2-amino-4-(1-piperidine) pyridine derivatives as novel anti crizotinib-resistant ALK/ROS1 dual inhibitors. Eur J Med Chem. 2019 Oct 1;179:358-375.

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

ROS-ERS inducer 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。

ROS-ERS inducer 1 

ROS-ERS inducer 1 是一种 II 型 ICD (免疫原性细胞死亡) 诱导剂。ROS-ERS inducer 1 是一种源自 4,5-二芳基咪唑的 Pt(II)-N-杂环卡宾 (Pt(II)-NHC) 复合物。ROS-ERS inducer 1 成功诱导内质网应激 (ERS) 伴随活性氧 (ROS) 的产生，并最终导致 HCC 细胞中损伤相关分子模式 (DAMP) 的释放。ROS-ERS inducer 1 显示出比 Cisplatin 高得多的抗癌活性。

ROS-ERS inducer 1

ROS-ERS inducer 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

ROS-ERS inducer 1 is a type II ICD (immunogenic cell death) inducer. ROS-ERS inducer 1 is a Pt(II)-N-heterocyclic carbene (Pt(II)-NHC) complex derived from 4,5-diarylimidazole. ROS-ERS inducer 1 successfully induces endoplasmic reticulum stress (ERS) accompanied by reactive oxygen species (ROS) generation and finally lead to the release of damage-associated molecular patterns (DAMPs) in HCC cells. ROS-ERS inducer 1 displays much higher anticancer activities than Cisplatin[1].

分子量

841.36

Formula

C24H24F2I2N3Pt
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]. Bian M, et al. Pt(II)-NHC Complex Induces ROS-ERS-Related DAMP Balance to Harness Immunogenic Cell Death in Hepatocellular Carcinoma. J Med Chem. 2022;65(3):1848-1866.

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

ROS-ERS inducer 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。

ROS-ERS inducer 1 

ROS-ERS inducer 1 是一种 II 型 ICD (免疫原性细胞死亡) 诱导剂。ROS-ERS inducer 1 是一种源自 4,5-二芳基咪唑的 Pt(II)-N-杂环卡宾 (Pt(II)-NHC) 复合物。ROS-ERS inducer 1 成功诱导内质网应激 (ERS) 伴随活性氧 (ROS) 的产生，并最终导致 HCC 细胞中损伤相关分子模式 (DAMP) 的释放。ROS-ERS inducer 1 显示出比 Cisplatin 高得多的抗癌活性。

ROS-ERS inducer 1

ROS-ERS inducer 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

ROS-ERS inducer 1 is a type II ICD (immunogenic cell death) inducer. ROS-ERS inducer 1 is a Pt(II)-N-heterocyclic carbene (Pt(II)-NHC) complex derived from 4,5-diarylimidazole. ROS-ERS inducer 1 successfully induces endoplasmic reticulum stress (ERS) accompanied by reactive oxygen species (ROS) generation and finally lead to the release of damage-associated molecular patterns (DAMPs) in HCC cells. ROS-ERS inducer 1 displays much higher anticancer activities than Cisplatin[1].

分子量

841.36

Formula

C24H24F2I2N3Pt
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]. Bian M, et al. Pt(II)-NHC Complex Induces ROS-ERS-Related DAMP Balance to Harness Immunogenic Cell Death in Hepatocellular Carcinoma. J Med Chem. 2022;65(3):1848-1866.

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

ROS-ERS inducer 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。

ROS-ERS inducer 1 

ROS-ERS inducer 1 是一种 II 型 ICD (免疫原性细胞死亡) 诱导剂。ROS-ERS inducer 1 是一种源自 4,5-二芳基咪唑的 Pt(II)-N-杂环卡宾 (Pt(II)-NHC) 复合物。ROS-ERS inducer 1 成功诱导内质网应激 (ERS) 伴随活性氧 (ROS) 的产生，并最终导致 HCC 细胞中损伤相关分子模式 (DAMP) 的释放。ROS-ERS inducer 1 显示出比 Cisplatin 高得多的抗癌活性。

ROS-ERS inducer 1

ROS-ERS inducer 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

ROS-ERS inducer 1 is a type II ICD (immunogenic cell death) inducer. ROS-ERS inducer 1 is a Pt(II)-N-heterocyclic carbene (Pt(II)-NHC) complex derived from 4,5-diarylimidazole. ROS-ERS inducer 1 successfully induces endoplasmic reticulum stress (ERS) accompanied by reactive oxygen species (ROS) generation and finally lead to the release of damage-associated molecular patterns (DAMPs) in HCC cells. ROS-ERS inducer 1 displays much higher anticancer activities than Cisplatin[1].

分子量

841.36

Formula

C24H24F2I2N3Pt
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]. Bian M, et al. Pt(II)-NHC Complex Induces ROS-ERS-Related DAMP Balance to Harness Immunogenic Cell Death in Hepatocellular Carcinoma. J Med Chem. 2022;65(3):1848-1866.

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