XL-647

Research use only, not for human use.

XL-647 (Tesevatinib, EXEL-7647, KD-019) is a novel spectrum-selective kinase inhibitor that potently inhibits the EGFR, ErbB2, KDR and EphB4 with IC50 of 0.3, 16, 1.5 and 1.4 nM, respectively.

XL-647 (Tesevatinib, EXEL-7647, KD-019) is a novel spectrum-selective kinase inhibitor that potently inhibits the EGFR, ErbB2, KDR and EphB4 with IC50 of 0.3, 16, 1.5 and 1.4 nM, respectively; shows no inhibition on IGF1R and InsR, also is inactive against a panel of 55 serine-threonine kinases (including CDKs, stress-activated protein kinases, and PKC isoforms; inhibits WT and mutant EGFR phosphorylation in cells with IC50 of 5 and 74 nM, inhibits mutant EGFR resistant to gefitinib and erlotinib, inhibits cellular proliferation and EGFR pathway activation in the erlotinib-resistant H1975 cell line that harbors double mutation L858R/T790M; inhibits H1975 xenograft tumors and reduces both tumor EGFR signaling and tumor vessel density in vivo.Lung Cancer Phase 3 Clinical

Tesevatinib;EXEL-7647;KD-019

Angiogenesis

EGFR

EGFR

Cancer

Lung Cancer

781613-23-8

491.40

C24H25Cl2FN4O2

>98% (HPLC)

DMSO: ≥ 30 mg/mL

O=C(NC1=CC=C(CCN2CC3=C(C=C(OC)C(OC)=C3)CC2)C=C1)C4=CC=CC(/C=C(C(N(C)/C5=C\C6=CC=CC=C6)=O)\NC5=O)=C4

4-Quinazolinamine, N-(3,4-dichloro-2-fluorophenyl)-6-methoxy-7-[[(3aα,5β,6aα)-octahydro-2-methylcyclopenta[c]pyrrol-5-yl]methoxy]-

(-20℃)

With Ice Pack

≥ 2 years