XMD8-87

Research use only, not for human use.

XMD8-87 (Ack1 inhibitor B19) is a potent Ack1 inhibitor with Kd of 15 nM, inhibits EGF-induced autophosphorylation in HEK293 cells at 2 uM.

XMD8-87 (Ack1 inhibitor B19) is a potent Ack1 inhibitor with Kd of 15 nM, inhibits EGF-induced autophosphorylation in HEK293 cells at 2 uM; completely inhibits A549 cancer cell growth, and partially inhibited EGF-stimulated cancer cell growth at 10 uM; XMD8-87 is a potent, selective Ack1 (TNK2) inhibitor with IC50 of 1.9 uM in ELISA assays; potently block proliferation of TNK2 mutant cell lines, shows IC50s of 38 nM and 113 nM for the D163E and R806Q mutations.(In Vitro):XMD8-87 potently inhibits the growth of the TNK2 mutant expressing cell lines while having little or no effect on the control cells out to the highest tested concentrations (1,000 nM). XMD8-87 has IC50s of 38 nM and 113 nM for the D163E and R806Q mutations. The effects of XMD8-87 on TNK2 cell lines are largely due to on-target effects on TNK2. Auto-phosphorylation of overexpressed TNK2 mutants could be blocked with TNK2 inhibitor XMD8-87.

XMD8-87 potently inhibits the growth of the TNK2 mutant expressing cell lines while having little or no effect on the control cells out to the highest tested concentrations (1,000 nM). XMD8-87 has IC50s of 38 nM and 113 nM for the D163E and R806Q mutations. The effects of XMD8-87 on TNK2 cell lines are largely due to on-target effects on TNK2. Auto-phosphorylation of overexpressed TNK2 mutants could be blocked with TNK2 inhibitor XMD8-87.

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Ack1 inhibitor B19

Tyrosine Kinase

Ack1 (TNK2)

TNK2

Cancer

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1234480-46-6

445.527

C24H27N7O2

>98% (HPLC)

DMSO: 65 mg/mL (145.89 mM)Ethanol: 5 mg/mL (11.2 mM)Water: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

C1=NC(NC2=CC=C(N3CCN(C)CC3)C=C2OC)=NC2N(C)C3C=CC=CC=3C(=O)NC1=2

2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-11-methyl-5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one

(-20℃)

With Ice Pack

≥ 2 years