IHMT-TRK-284

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。

IHMT-TRK-284 

IHMT-TRK-284 (Compound 34) 是一种有效的、具有口服活性的 type II TRK kinase 抑制剂,对 TRKA, B, CIC50 值分别为 10.5, 0.7和2.6 nM。 IHMT-TRK-284 在激酶组中表现出良好的选择性、具有良好的体内抗肿瘤效果。

IHMT-TRK-284

IHMT-TRK-284 Chemical Structure

CAS No. : 2416844-79-4

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生物活性

IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies[1].

IC50 & Target

TrkB

0.7 nM (IC50)

TrkC

2.6 nM (IC50)

TrkA

10.5 nM (IC50)

PDGFRα

24.2 nM (IC50)

PDGFRβ

95.7 nM (IC50)

Abl1

83.6 nM (IC50)

CSF1R

1.2 nM (IC50)

KIT

2167 nM (IC50)

体外研究
(In Vitro)

IHMT-TRK-284 (Compound 34) (0-10 µM, 72 h) shows antiproliferative effects against BaF3 cells, a panel of kinase transformed BaF3 cells, and KM-12-LUC cells[1].
IHMT-TRK-284 (0-10 µM, 24 h) induces apoptosis and arrests the cell cycle into G0/G1 phase in KM-12-LUC cells[1].
IHMT-TRK-284 exerts its inhibitory effect to the colon cancer cells through on-target inhibition of TRK[1].
IHMT-TRK-284 could overcome drug resistant mutants including V573M and F589L in the ATP binding pocket as well as G667C/S in the DFG region[1].
IHMT-TRK-284 shows selectivity over VEGFR2 kinase[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: BaF3 cells, a panel of kinase transformed BaF3 cells, and KM-12-LUC cells
Concentration: 0-10 µM
Incubation Time: 72 h
Result: Showed antiproliferative effects against BaF3 cells, a panel of kinase transformed BaF3 cells, and KM-12-LUC cells. GI50 for KM-12-LUC cells was 0.002 µM.
Antiproliferative effects of IHMT-TRK-284 against a panel of kinase transformed BaF3 cells[1].

Target GI50 (nM)
BaF3-TEL-ABL 411.1
BaF3-TEL-CSF1R 4
BaF3-TEL-KIT 923.2
BaF3-TEL-PDGFRα 1.7
BaF3-TEL-PDGFRβ 1.4
BaF3-TEL-TRKA 8.5
BaF3-TEL-TRKB 8.2
BaF3-TEL-TRKC 27.3
BaF3-TEL-VEGFR2 1180


Antiproliferative effects of IHMT-TRK-284 against a panel of TRKs wt/mutants transformed BaF3 cells (n = 3)[1].

Cells GI50 (µM)
BaF3 1.4 ± 0.011
BaF3-LMNA-TRKA 0.007 ± 0.001
BaF3-LMNA-TRKA-V573M 0.003 ± 0.001
BaF3-LMN

Western Blot Analysis[1]

Cell Line: BaF3-TEL-TRKA, BaF3-TEL-TRKB, BaF3-TEL-TRKC, BaF3-LMNATRKA-V573M, BaF3-LMNA-TRKA-F589L, BaF3-LMNA-TRKA-G595R, BaF3-LMNA-TRKA-G667C/S, and KM-12-LUC cells
Concentration: 0, 0.01, 0,03, 0.1, 0.3, 1, 3, and 10 µM
Incubation Time: 2 h
Result: In transformed BaF3 cells: Inhibited the phosphorylation of TRKA Y490 (EC50 = 0.026 µM) and corresponding tyrosine residues TRKB Y515 (EC50 = 0.069 µM) and TRKC Y516 (EC50 = 0.029 µM); potently inhibited the phosphorylation of Y490 in V573M, F589L, and G667C/S mutants with EC50s of 0.013 µM, 0.021 µM, 0.067 µM, and 0.074 µM respectively. In KM-12-LUC cells: Blocked the phosphorylation of TRKA Y490 at the concentration of 0.01 µM; remarkably inhibited the phosphorylation of downstream signaling mediators AKT T308/S473 and ERK1/2 (T202/Y204) (EC50 less than 0.03 µM).

Apoptosis Analysis[1]

Cell Line: KM-12-LUC cells
Concentration: 0, 0.01, 0,03, 0.1, 0.3, 1, 3, and 10 µM
Incubation Time: 24 h
Result: Induced dose-dependent cell apoptotic death.

Cell Cycle Analysis[1]

Cell Line: KM-12-LUC cells
Concentration: 0, 0.01, 0,03, 0.1, 0.3, 1, 3, and 10 µM
Incubation Time: 24 h
Result: Arrested the cell cycle into G0/G1 phase.

体内研究
(In Vivo)

IHMT-TRK-284 (Compound 34) (40 and 80 mg/kg; p.o.; daily, 10 days) shows good in vivo PK and antitumor efficacy properties[1].

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

Animal Model: Four-week old female nu/nu mice, one million BaF3-TELTRKA, BaF3-TEL-TRKB, BaF3-TEL-TRKC, BaF3-LMNA-TRKA-F589L, BaF3-LMNA-TRKA-G667S, and five million KM-12-LUC cells in DMEM medium were formulated as a 1:1 mixture with matrigel and injected into the subcutaneous space on the right flank of nu/nu mice[1]
Dosage: 40 mg/kg and 80 mg/kg
Administration: Daily oral gavage, 10 days
Result: Dose-dependently inhibited the BaF3-TEL-TRKA, BaF3-TEL-TRKB, and BaF3-TEL-TRKC tumor progression with TGI (tumor growth inhibition) of 68%, 93%, and 58%. Dose-dependently inhibited the tumor progression and exhibited the TGI of 93% at 40 mg/kg/day and 95% at 80 mg/kg/day in KM-12-LUC cells inoculated xenograft mouse model. Potently inhibited the tumor growth with TGI values of 88% and 89% respectively at 80 mg/kg dosage in BaF3- LMNA-TRKA-F589L and BaF3-LMNA-TRKA-G667S cells.
Animal Model: Mice, sprague dawley rats, and beagle dogs[1]
Dosage: 1 mg/kg and 10 mg/kg
Administration: Intravenous injection and oral administration (Pharmacokinetic Analysis)
Result: Pharmacokinetic study of IHMT-TRK-284 in mice, sprague dawley rats, and beagle dogsa[1]

Parameter Mice
i.v. (1 mg/kg)
Mice
p.o. (10 mg/kg)
Rats
i.v. (1 mg/kg)
Rats
p.o. (10 mg/kg)
Beagle Dogs
i.v. (1 mg/kg)
Beagle Dogs
p.o. (10 mg/kg)
AUC(0-t)
(ng/mL*h)
748 1431 393 952 323 464
Tmax (h) 0.033 1.5 0.03 4.7 0.08 4.3
T1/2 (h) 2.6 3.4 2.7 2.5 0.03 11.8
Vz (mL/kg) 4934 31567 9682

分子量

473.59

Formula

C25H27N7OS

CAS 号

2416844-79-4

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]. Beilei Wang, et al. Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants. Eur J Med Chem. 2020 Dec 1;207:112744.

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DDR-TRK-1

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。

DDR-TRK-1 

DDR-TRK-1 是圆盘状受体 1 (DDR1) 的一个选择性抑制剂,其 IC50 值为 9.4 nM。DDR-TRK-1 也抑制 TRK 激酶家族。

DDR-TRK-1

DDR-TRK-1 Chemical Structure

CAS No. : 1934246-19-1

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生物活性

DDR-TRK-1 is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR-TRK-1 also inhibits TRK family.

IC50 & Target

IC50: 9.4 nM (DDR1)[1].

体外研究
(In Vitro)

DDR-TRK-1 is a promising candidate, with an IC50 value of 9.4 nM against DDR1. DDR-TRK-1 also exhibits reasonable pharmacokinetic (PK) properties, with an oral bioavailability of 66.8% and a T1/2 value of 1.25 h at an oral dose of 20 mg/kg in rats. However, the area under concentration−time curve (AUC) value of DDR-TRK-1 in mice is obviously higher than that in rats, suggesting its good absorption property in mice. The DDR1 inhibition of DDR1-IN-3 is further validated by determining its binding affinity with the DDR1 protein. It is shown that DDR-TRK-1 bounds tightly to DDR1, with a binding constant (Kd) value of 4.7 nM[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.

体内研究
(In Vivo)

DDR-TRK-1 prevents these BLM-induced pathological changes in a dose-dependent manner. These results agree with the expression levels of fibrotic markers in lung tissue lysates, including fibronectin and α-smooth muscle actin (SMA). Further analyses also reveal that the administration of DDR-TRK-1 cause a dose-dependent suppression in the content of hydroxyproline, a unique amino acid found in collagen. The above data collectively indicate the promising therapeutic potential of DDR-TRK-1 against the BLM-induced pulmonary fibrosis[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

492.50

Formula

C26H23F3N6O

CAS 号

1934246-19-1

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]. Zhen Wang, et al. Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors. J Med Chem. 2016 Jun 23; 59(12): 5911–5916.

Cell Assay
[1]

Panc-1 cells are plated at low density in media in the presence or absence of controls or the indicated concentration of DDR-TRK-1 (0.016, 0.0625, 0.25, 1 μM). Colony formation is evaluated after 1.5-2 weeks by fixing and staining with crystal violet. The effect of DDR1-IN-3 on cell migration is determined through a ‘scratch’ assay. Panc-1 cells are grown to confluence in a 6 well dish. A scratch is made using a p20 pipette tip and cell migration into the wound is determined at 12, 24, 48, 60, and 72 hrs. The effect of control compounds or DDR-TRK-1 at the indicated concentrations is determined at each time point[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 Administration
[1]

Mice[1]
To induce pulmonary damage, 6- to 8-week-old sex- and age-matched wild type or slie mice (at least five animals per group) are intranasally dropped with bleomycin at 5mg/kg BW. The inhibitors (e.g., DDR-TRK-1) are dissolved in water at a concentration of 5 mg/mL and given to the mice orally by gavage twice a day. Hydroxyproline accounts for 13.4% of the total amino acids of collagen; thus its content can be used to reflect the severity of fibrosis. A commercial hydroxyproline kit is used. Briefly, fresh lung tissues are weighted and hydrolyzed to release hydroxyproline. After a series of chemical reactions, a pink color solution is formed and then subjected to measurement of absorbance at 560 nm. The hydroxyproline content of each sample is calculated by comparing with the standards[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.

参考文献
  • [1]. Zhen Wang, et al. Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors. J Med Chem. 2016 Jun 23; 59(12): 5911–5916.

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Trk-IN-6

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。

Trk-IN-6 

Trk-IN-6 在体外对 TRK 突变体显示出极好的效力(IC50 = 0.2-0.7 nM)。

Trk-IN-6

Trk-IN-6 Chemical Structure

CAS No. : 2489327-43-5

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生物活性

Trk-IN-6 shows excellent in vitro potency on a panel of TRK mutants (IC50 = 0.2-0.7 nM).

分子量

446.43

Formula

C21H21F3N6O2

CAS 号

2489327-43-5

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]. Zhuo LS, et al. Discovery of Next-Generation Tropomyosin Receptor Kinase Inhibitors for Combating Multiple Resistance Associated with Protein Mutation. J Med Chem. 2021 Oct 28;64(20):15503-15514.

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Trk-IN-6

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。

Trk-IN-6 

Trk-IN-6 在体外对 TRK 突变体显示出极好的效力(IC50 = 0.2-0.7 nM)。

Trk-IN-6

Trk-IN-6 Chemical Structure

CAS No. : 2489327-43-5

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生物活性

Trk-IN-6 shows excellent in vitro potency on a panel of TRK mutants (IC50 = 0.2-0.7 nM).

分子量

446.43

Formula

C21H21F3N6O2

CAS 号

2489327-43-5

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]. Zhuo LS, et al. Discovery of Next-Generation Tropomyosin Receptor Kinase Inhibitors for Combating Multiple Resistance Associated with Protein Mutation. J Med Chem. 2021 Oct 28;64(20):15503-15514.

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Trk-IN-6

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。

Trk-IN-6 

Trk-IN-6 在体外对 TRK 突变体显示出极好的效力(IC50 = 0.2-0.7 nM)。

Trk-IN-6

Trk-IN-6 Chemical Structure

CAS No. : 2489327-43-5

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250 mg   询价  
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生物活性

Trk-IN-6 shows excellent in vitro potency on a panel of TRK mutants (IC50 = 0.2-0.7 nM).

分子量

446.43

Formula

C21H21F3N6O2

CAS 号

2489327-43-5

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]. Zhuo LS, et al. Discovery of Next-Generation Tropomyosin Receptor Kinase Inhibitors for Combating Multiple Resistance Associated with Protein Mutation. J Med Chem. 2021 Oct 28;64(20):15503-15514.

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TRK-IN-19

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。

TRK-IN-19 

TRK-IN-19 (Compound I-10 ) 是一种有效的 TRK 抑制剂 (TRKA IC50 = 1.1 nM, TRKA G595R IC50 = 5.3 nM)。TRK-IN-19 具有研究癌症疾病的潜力。

TRK-IN-19

TRK-IN-19 Chemical Structure

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生物活性

TRK-IN-19 (Compound I-10 ) is a potent inhibitor of TRK (TRKA IC50 = 1.1 nM, TRKAG595R IC50 = 5.3 nM). TRK-IN-19 has the potential for the research of cancer diseases[1].

分子量

411.47

Formula

C22H26FN5O2

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]. Sun M, et al. Design, synthesis and biological activity of bicyclic carboxamide derivatives as TRK inhibitors. Bioorg Med Chem. 2020 Dec 1;28(23):115811. doi: 10.1016/j.bmc.2020.115811.

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Pan-Trk-IN-3

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。

Pan-Trk-IN-3 

Pan-Trk-IN-3 (Compound 11g) 是一种有效的广谱 Trk 及其耐药突变体抑制剂。对 TrkATrkBTrkCTrkAG595RTrkAG667CTrkAG667STrkAF589LTrkCG623RIC50 分别为 2、3、2、21、26、5、7 和 6 nM。Pan-Trk-IN-3 表现出极好的抗肿瘤活性,诱导细胞凋亡 (apoptosis)。

Pan-Trk-IN-3

Pan-Trk-IN-3 Chemical Structure

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生物活性

Pan-Trk-IN-3 (Compound 11g) is a potent inhibitor of pan-Trk and their drug-resistant mutants with IC50 values of 2, 3, 2, 21, 26, 5, 7 and 6 nM against TrkA, TrkB, TrkC, TrkAG595R, TrkAG667C, TrkAG667S, TrkAF589L and TrkCG623R, respectively. Pan-Trk-IN-3 displays excellent antitumor activity and induces apoptosis[1].

IC50 & Target

TrkA

2 nM (IC50)

TrkC

2 nM (IC50)

TrkB

3 nM (IC50)

TrkAG667S

5 nM (IC50)

TrkCG623R

6 nM (IC50)

TrkAF589L

7 nM (IC50)

TrkAG595R

21 nM (IC50)

TrkAG667C

26 nM (IC50)

分子量

575.06

Formula

C29H31ClN8O3

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]. Pan S,et al. Structural Optimization and Structure-Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6H-pyrimido[5,4-b][1,4]oxazin-7(8H)-one Derivatives as A New Class of Potent Inhibitors of Pan-Trk and Their Drug-Resistant Mutants. J Med Chem. 2022 Feb 10;65(3):2035-2058.

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Pan-Trk-IN-2

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。

Pan-Trk-IN-2 

化合物Cpd-1是一种小分子 Trks 抑制剂,具有良好的抗肿瘤活性。

Pan-Trk-IN-2

Pan-Trk-IN-2 Chemical Structure

CAS No. : 2583778-77-0

规格 是否有货
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生物活性

Compound cpd-1 is a small molecule Trks inhibitor with good antitumor activity[1].

分子量

506.86

Formula

C22H18ClF3N6O3

CAS 号

2583778-77-0

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]. Pan S,et al. Structural Optimization and Structure-Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6H-pyrimido[5,4-b][1,4]oxazin-7(8H)-one Derivatives as A New Class of Potent Inhibitors of Pan-Trk and Their Drug-Resistant Mutants. J Med Chem. 2022 Feb 10;65(3):2035-2058.

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TRK-IN-14

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。

TRK-IN-14 

TRK-IN-14 是一种有效的 TRK 抑制剂。蛋白激酶在控制细胞生长和分化中起关键作用,并负责控制多种细胞信号转导过程。TRK-IN-14 具有研究 TRK 相关疾病的潜力 (摘自专利 WO2012034091A1,化合物 X-47)。

TRK-IN-14

TRK-IN-14 Chemical Structure

CAS No. : 1365212-84-5

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生物活性

TRK-IN-14 is a potent inhibitor of TRK. Protein kinases play a critical role in the control of cell growth and differentiation and are responsible for the control of a wide variety of cellular signal transduction processes. TRK-IN-14 has the potential for the research of TRK-related diseases (extracted from patent WO2012034091A1, compound X-47)[1].

分子量

433.45

Formula

C24H21F2N5O

CAS 号

1365212-84-5

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]. Yi Fan, et al. Imidazo [1, 2] pyridazin compounds and compositions as trk inhibitors. Patent WO2012034091A1.

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TRK-IN-16

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。

TRK-IN-16 

TRK-IN-16 是一种有效的 TRK 抑制剂。蛋白激酶在控制细胞生长和分化中起关键作用,并负责控制多种细胞信号转导过程。TRK-IN-16 具有研究 TRK 相关疾病的潜力(摘自专利 WO2012034091A1,化合物 X-21)。

TRK-IN-16

TRK-IN-16 Chemical Structure

CAS No. : 1365212-81-2

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生物活性

TRK-IN-16 is a potent inhibitor of TRK. Protein kinases play a critical role in the control of cell growth and differentiation and are responsible for the control of a wide variety of cellular signal transduction processes. TRK-IN-16 has the potential for the research of TRK-related diseases (extracted from patent WO2012034091A1, compound X-21)[1].

分子量

353.39

Formula

C19H20FN5O

CAS 号

1365212-81-2

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]. Yi Fan, et al. Imidazo [1, 2] pyridazin compounds and compositions as trk inhibitors. Patent WO2012034091A1.

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TRK-IN-18

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。

TRK-IN-18 

TRK-IN-18 是一种有效的 TRK 抑制剂。原肌球蛋白相关激酶 (Trks) 是由神经营养因子激活的受体酪氨酸激酶家族,神经营养因子是一组可溶性生长因子,包括神经生长因子 (NGF)、脑源性神经营养因子 (BDNF) 和神经营养因子-3 (NT-3),以及 神经营养因子-4/5 (NT-4/5)。TRK-IN-18 具有研究癌症疾病的潜力(摘自专利 WO2021148805A1,化合物 7)。

TRK-IN-18

TRK-IN-18 Chemical Structure

CAS No. : 2412008-91-2

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生物活性

TRK-IN-18 is a potent inhibitor of TRK. Tropomyosin-related kinases (Trks) are a family of receptor tyrosine kinases activated by neurotrophins, a group of soluble growth factors including Nerve Growth Factor (NGF), Brain-Derived Neurotrophic Factor (BDNF) and Neurotrophin-3 (NT-3) and Neurotrophin-4/5 (NT-4/5). TRK-IN-18 has the potential for the research of cancer diseases (extracted from patent WO2021148805A1, compound 7)[1].

分子量

495.54

Formula

C25H23F2N5O2S

CAS 号

2412008-91-2

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]. Nicola ROBAS, et al. Topical pharmaceutical compositions comprising imidazo[1,2-b]pyridazine compounds. Paatent WO2021148805A1.

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TRK-IN-13

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。

TRK-IN-13 

TRK-IN-13 是一种有效的 TRK 抑制剂。蛋白激酶在控制细胞生长和分化中起关键作用,并负责控制多种细胞信号转导过程。TRK-IN-13 具有研究 TRK 相关疾病的潜力 (摘自专利 WO2012034091A1,化合物 X-24)。

TRK-IN-13

TRK-IN-13 Chemical Structure

CAS No. : 1365221-52-8

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生物活性

TRK-IN-13 is a potent inhibitor of TRK. Protein kinases play a critical role in the control of cell growth and differentiation and are responsible for the control of a wide variety of cellular signal transduction processes. TRK-IN-13 has the potential for the research of TRK-related diseases (extracted from patent WO2012034091A1, compound X-24)[1].

分子量

433.45

Formula

C24H21F2N5O

CAS 号

1365221-52-8

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]. Yi Fan, et al. Imidazo [1, 2] pyridazin compounds and compositions as trk inhibitors. Patent WO2012034091A1.

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TRK/ALK-IN-1

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。

TRK/ALK-IN-1 

TRK/ALK-IN-1 (compound 21) 是一种有效的 TRKALK 双重抑制剂。TRK/ALK-IN-1 在酶促测定中与抗增殖活性非常吻合,对 TRKA、ALKIC50 值分别为 2.2、9.3 和 38 nM< sup>WT 和 ALKL1196M。TRK/ALK-IN-1具有研究癌症疾病的潜力。

TRK/ALK-IN-1

TRK/ALK-IN-1 Chemical Structure

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生物活性

TRK/ALK-IN-1 (compound 21) is a potent and dual inhibitor of TRK and ALK. TRK/ALK-IN-1 in the enzymatic assays is in good accordance with anti-proliferative activity with IC50 values of 2.2, 9.3 and 38 nM towards TRKA, ALKWT and ALKL1196M, respectively. TRK/ALK-IN-1 has the potential for the research of cancer diseases[1].

分子量

657.18

Formula

C31H35ClF2N8O2S

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]. Li T, et al. Discovery of novel 2-phenylamino-4-prolylpyrimidine derivatives as TRK/ALK dual inhibitors with promising antitumor effects. Bioorg Med Chem. 2021 Oct 1;47:116396.

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TRK-IN-15

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。

TRK-IN-15 

TRK-IN-15 是一种有效的 TRK 抑制剂。蛋白激酶在控制细胞生长和分化中起关键作用,并负责控制多种细胞信号转导过程。TRK-IN-15 具有研究 TRK 相关疾病的潜力 (摘自专利 WO2012034091A1,化合物 X-55)。

TRK-IN-15

TRK-IN-15 Chemical Structure

CAS No. : 1365213-20-2

规格 是否有货
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生物活性

TRK-IN-15 is a potent inhibitor of TRK. Protein kinases play a critical role in the control of cell growth and differentiation and are responsible for the control of a wide variety of cellular signal transduction processes. TRK-IN-15 has the potential for the research of TRK-related diseases (extracted from patent WO2012034091A1, compound X-55)[1].

分子量

353.39

Formula

C19H20FN5O

CAS 号

1365213-20-2

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]. Yi Fan, et al. Imidazo [1, 2] pyridazin compounds and compositions as trk inhibitors. Patent WO2012034091A1.

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

TRK-IN-17

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。

TRK-IN-17 

TRK-IN-17 是一种有效的 TRK 抑制剂。原肌球蛋白相关激酶 (Trks) 是由神经营养因子激活的受体酪氨酸激酶家族,神经营养因子是一组可溶性生长因子,包括神经生长因子 (NGF)、脑源性神经营养因子 (BDNF) 和神经营养因子-3 (NT-3),以及神经营养因子-4/5 (NT-4/5)。TRK-IN-17具有研究癌症疾病的潜力(摘自专利 WO2021148807A1,化合物 3)。

TRK-IN-17

TRK-IN-17 Chemical Structure

CAS No. : 2409544-80-3

规格 是否有货
100 mg   询价  
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500 mg   询价  

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生物活性

TRK-IN-17 is a potent inhibitor of TRK. Tropomyosin-related kinases (Trks) are a family of receptor tyrosine kinases activated by neurotrophins, a group of soluble growth factors including Nerve Growth Factor (NGF), Brain-Derived Neurotrophic Factor (BDNF) and Neurotrophin-3 (NT-3) and Neurotrophin-4/5 (NT-4/5). TRK-IN-17 has the potential for the research of cancer diseases (extracted from patent WO2021148807A1, compound 3)[1].

分子量

441.50

Formula

C21H21F2N7S

CAS 号

2409544-80-3

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]. Nicola ROBAS, et al. Pharmaceutical compositions and their uses. Patent WO2021148807A1.

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Trk-IN-7

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。

Trk-IN-7 

Trk-IN-7 (compound I-6) 是一种有效的 Trk 抑制剂,对 TRKA、TRKB 和 TRKC的 IC50 分别为0.25-10 nM。Trk-IN-7 对 EML4-ALK (IC50<15 nm)、alk g1202r、alk c1156y、alk r1275q、alk f1174l、alk l1197m 和 alk g1269a (IC50=5-50 nM) 有抑制作用。

Trk-IN-7

Trk-IN-7 Chemical Structure

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生物活性

Trk-IN-7 (compound I-6) is a potent TRK inhibitor with IC50s of ranging from 0.25-10 nM for TRKA, TRKB and TRKC, respectively. Trk-IN-7 shows inhibition against EML4-ALK (IC50<15 nm) alk g1202r, c1156y, r1275q, f1174l, l1197m, and g1269a (IC50=5-50 nM)[1].

IC50 & Target[1]

TrkA

<25 nM (IC50)

TrkB

<5 nM (IC50)

TrkC

<25 nM (IC50)

分子量

368.36

Formula

C18H17FN6O2

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]. Diaryl macrocyclic compound as protein kinase modulator. WO2019210835A1.

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

Trk-IN-8

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。

Trk-IN-8 

Trk-IN-8 是一种有效的 TRKA 抑制剂,对 TRKAa、TRKA(G595R) 和 TRKC(G623R) 的 IC50 分别为 0.42、0.89 和 1.5 nM (WO2021115401A1, compound 3)。

Trk-IN-8

Trk-IN-8 Chemical Structure

规格 是否有货
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生物活性

Trk-IN-8 is a potent TRK inhibitor with IC50s of 0.42, 0.89 and 1.5 nM for TRKAa, TRKA(G595R) and TRKC(G623R), respectively (WO2021115401A1, compound 3)[1].

分子量

386.36

Formula

C18H16F2N6O2

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]. Fluorine-containing heterocyclic derivatives with macrocyclic structure and use thereof. WO2021115401A1.

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

Trk-IN-7

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。

Trk-IN-7 

Trk-IN-7 (compound I-6) 是一种有效的 Trk 抑制剂,对 TRKA、TRKB 和 TRKC的 IC50 分别为0.25-10 nM。Trk-IN-7 对 EML4-ALK (IC50<15 nm)、alk g1202r、alk c1156y、alk r1275q、alk f1174l、alk l1197m 和 alk g1269a (IC50=5-50 nM) 有抑制作用。

Trk-IN-7

Trk-IN-7 Chemical Structure

规格 是否有货
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生物活性

Trk-IN-7 (compound I-6) is a potent TRK inhibitor with IC50s of ranging from 0.25-10 nM for TRKA, TRKB and TRKC, respectively. Trk-IN-7 shows inhibition against EML4-ALK (IC50<15 nm) alk g1202r, c1156y, r1275q, f1174l, l1197m, and g1269a (IC50=5-50 nM)[1].

IC50 & Target[1]

TrkA

<25 nM (IC50)

TrkB

<5 nM (IC50)

TrkC

<25 nM (IC50)

分子量

368.36

Formula

C18H17FN6O2

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]. Diaryl macrocyclic compound as protein kinase modulator. WO2019210835A1.

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

Trk-IN-8

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。

Trk-IN-8 

Trk-IN-8 是一种有效的 TRKA 抑制剂,对 TRKAa、TRKA(G595R) 和 TRKC(G623R) 的 IC50 分别为 0.42、0.89 和 1.5 nM (WO2021115401A1, compound 3)。

Trk-IN-8

Trk-IN-8 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
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生物活性

Trk-IN-8 is a potent TRK inhibitor with IC50s of 0.42, 0.89 and 1.5 nM for TRKAa, TRKA(G595R) and TRKC(G623R), respectively (WO2021115401A1, compound 3)[1].

分子量

386.36

Formula

C18H16F2N6O2

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]. Fluorine-containing heterocyclic derivatives with macrocyclic structure and use thereof. WO2021115401A1.

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

Trk-IN-7

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。

Trk-IN-7 

Trk-IN-7 (compound I-6) 是一种有效的 Trk 抑制剂,对 TRKA、TRKB 和 TRKC的 IC50 分别为0.25-10 nM。Trk-IN-7 对 EML4-ALK (IC50<15 nm)、alk g1202r、alk c1156y、alk r1275q、alk f1174l、alk l1197m 和 alk g1269a (IC50=5-50 nM) 有抑制作用。

Trk-IN-7

Trk-IN-7 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

Trk-IN-7 (compound I-6) is a potent TRK inhibitor with IC50s of ranging from 0.25-10 nM for TRKA, TRKB and TRKC, respectively. Trk-IN-7 shows inhibition against EML4-ALK (IC50<15 nm) alk g1202r, c1156y, r1275q, f1174l, l1197m, and g1269a (IC50=5-50 nM)[1].

IC50 & Target[1]

TrkA

<25 nM (IC50)

TrkB

<5 nM (IC50)

TrkC

<25 nM (IC50)

分子量

368.36

Formula

C18H17FN6O2

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]. Diaryl macrocyclic compound as protein kinase modulator. WO2019210835A1.

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