ALW-II-41-27

Research use only, not for human use.

ALW-II-41-27, an Eph receptor tyrosine kinase inhibitor, is used for cancer therapy.

ALW-II-41-27 is a Eph receptor tyrosine kinase inhibitor. pharmacologic inhibition of EPHA2 by the small-molecule inhibitor ALW-II-41-27 decreased both survival and proliferation of erlotinib-resistant tumor cells and inhibited tumor growth in vivo. ALW-II-41-27 was also effective in decreasing viability of cells with acquired resistance to the third-generation EGFR TKI AZD9291. Collectively, these data define a role for EPHA2 in the maintenance of cell survival of TKI-resistant, EGFR-mutant lung cancer and indicate that EPHA2 may serve as a useful therapeutic target in TKI-resistant tumors.

ALW-II-41-27 inhibits Ba/F3 cells transformed with Tel fusions of EphA3, Kit, Fms, KDR, FLT1, FGR, Src, Lyn, Bmx, and Bcr-Abl with an EC50?below 500 nM. ALW-II-41-27 exhibits cross reactivity with Bcr-Abl. ALW-II-41-27 inhibits b-raf, CSF1R, DDR1, DDR2, EphA2, EphA5, EphA8, EphB1, EphB2, EphB3, Frk, Kit, Lck, p38α, p38β, PDGFRα, PDGFRβ, and Raf1 and many more demonstrating how introduction of the thiophene group can have a tremendous impact on kinase selectivity.

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ALW-II-41-27 | ALW II-41-27 | ALWII-41-27

Microbiology/Virology

HIV

Ephrin Receptor

Cancer

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1186206-79-0

607.7

C32H32F3N5O2S

>98% (HPLC)

DMSO : ≥ 47 mg/mL. 77.34 mM

CC1=C(NC(C2=CC(C3=CC=CS3)=CN=C2)=O)C=C(C(NC4=CC=C(CN5CCN(CC)CC5)C(C(F)(F)F)=C4)=O)C=C1

N-(5-((4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)carbamoyl)-2-methylphenyl)-5-(thiophen-2-yl)nicotinamide

(-20℃)

With Ice Pack

≥ 2 years