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Chemical Structure : GNF-5837
CAS No.: 1033769-28-6
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $148 | In stock | |
| 50 mg | $248 | In stock | |
| 100 mg | $398 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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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.
| M.Wt | 535.503 | |
| Formula | C28H21F4N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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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