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Chemical Structure : DS-1205b
CAS No.: 1855860-24-0
Catalog No.: PC-38043Not For Human Use, Lab Use Only.
DS-1205b (DS1205b) is a potent, highly selective inhibitor of AXL kinase with IC50 of 1.3 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $248 | In stock | |
| 10 mg | $398 | In stock | |
| 50 mg | $898 | In stock | |
| 100 mg | $1480 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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DS-1205b (DS1205b) is a potent, highly selective inhibitor of AXL kinase with IC50 of 1.3 nM.
DS-1205b displays 48-, 80-, and 313-fold selectivity ovver MER, MET, and TRKA.
DS-1205b inhibits phosphorylation of AKT serine/threonine kinase in a dose-dependent manner.
DS-1205b does not obviously inhibit cell proliferation and viability in NIH3T3-AXL cells.
DS-1205b significantly suppresses cell migration on NIH3T3-AXL with IC50 of 2.7 nM.
DS-1205b induces tumor regression by 54-86% at doses of 6.3-50 mg/kg in mice bearing subcutaneously implanted NIH3T3-AXL cells.
DS-1205b inhibits AXL signaling in vitro when combined with erlotinib or osimertinib, delays erlotinib acquired resistance and restores the treatment effect of erlotinib in an HCC827 sc xenograft model.
| M.Wt | 735.81 | |
| Formula | C41H42FN5O7 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(R)-N-(4-(5-(4-((1,4-dioxan-2-yl)methoxy)-3-methoxyphenyl)-2-aminopyridin-3-yl)-3-fluorophenyl)-5-methyl-4'-oxo-1'-((tetrahydro-2H-pyran-4-yl)methyl)-1',4'-dihydro-[2,3'-bipyridine]-5'-carboxamide |
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1. Takeshi Jimbo, et al. Oncotarget. 2019 Aug 27;10(50):5152-5167.
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