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DS-1205b

Chemical Structure : DS-1205b

CAS No.: 1855860-24-0

DS-1205b (DS1205b)

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 735.81
Formula C41H42FN5O7
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

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

References

1. Takeshi Jimbo, et al. Oncotarget. 2019 Aug 27;10(50):5152-5167.

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