XL-647

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

XL-647（Tesevatinib、EXEL-7647、KD-019）是一种新型谱选择性激酶抑制剂，可有效抑制 EGFR、ErbB2、KDR 和 EphB4，IC50 分别为 0.3、16、1.5 和 1.4 nM。

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 (XL-647) potently inhibits the EGF/ErbB2, VEGF, and ephrin RTK families. Tesevatinib (XL-647) is a reversible and ATP competitive inhibitor. Tesevatinib (XL-647) was inactive against a panel of 10 tyrosine kinases (including the insulin and the insulin-like growth factor-1 receptor) and 55 serine-threonine kinases (including cyclin-dependent kinases, stress-activated protein kinases, and protein kinase C isoforms). Tesevatinib (XL-647) inhibits cellular proliferation and EGFR pathway activation in the erlotinib-resistant H1975 cell line that harbors a double mutation (L858R and T790M) in the EGFR gene. In A431 cells, Tesevatinib (XL-647) reduces cell viability with IC50 values of 13 nM.

Tesevatinib (XL-647) shows potent and long-lived inhibition of the WT EGFR in vivo. Tesevatinib (XL-647) substantially inhibits the growth of H1975 xenograft tumors and reduces both tumor EGFR signaling and tumor vessel density.

Tesevatinib | EXEL-7647 | KD-019

Angiogenesis

EGFR

EGFR

Cancer

Lung Cancer

781613-23-8

491.4

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