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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Trk Receptor-GNF-5837
GNF-5837

Chemical Structure : GNF-5837

CAS No.: 1033769-28-6

GNF-5837 (GNF5837)

货号: PC-49205Not For Human Use, Lab Use Only.

GNF-5837 (GNF5837) is a potent, selective, and orally bioavailable pan-TRK inhibitor with IC50 values of 11/9/7 nM against TRKA/B/C, respectively.

规格 价格 库存 数量
10 mg ¥880 In stock
25 mg ¥1280 In stock
50 mg ¥1980 In stock
100 mg ¥3280 In stock
250 mg Get quote

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GNF-5837 (GNF5837) is a potent, selective, and orally bioavailable pan-TRK inhibitor with IC50 values of 11/9/7 nM against TRKA/B/C, respectively.
GNF-5837 demonstrated potent antiproliferation activity with IC50 of 42 nM in Ba/F3 cells expressing TRKA and NGF, with no effect in parental Ba/F3 cells whose proliferation is dependent on IL-3.
GNF-5837 potently inhibited cell growth and proliferation of RIE cells expressing TRKA and NGF with IC50 of 17 nM.
GNF-5837 showed significant selectivity window for TRK over c-Kit and PDGFR in cellular assays (IC50>0.5 uM).
GNF-5837 (25-100mg, p.o.) demonstrated 72 and 100% tumor regression at 50 and 100 mg/kg in tumor xenografts derived from RIE cells expressing both TRKA and NGF.

物理化学性质&存储条件

分子量 535.503
分子式 C28H21F4N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(Z)-1-(3-((3-((1H-pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea

参考文献

1. Albaugh P, et al. ACS Med Chem Lett. 2012 Jan 1;3(2):140-5.

2. Kimura S, et al. Lung Cancer. 2018 Jun;120:98-107.

3. Chen Y, et al. Oncol Rep. 2019 Nov;42(5):2039-2048.

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