XL647 Inhibitor CAS No. 651031-01-5

Cat. No.	Name	Size	Price	Add Cart
KI0621	XL647	5 mg	$488
KI0621	XL647	10 mg	$768

Chemical Characteristic

Product Name	XL647
Synonyms	EXEL-7647
CAS No.	651031-01-5
Molecular Weight	491.39
Formula	C₂₄H₂₅Cl₂FN₄O₂
Chemical Name	N-(3,4-Dichloro-2-fluorophenyl)-6-methoxy-7-{[(3aR,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methoxy}-4-quinazolinamine
Smiles	n1cnc(c2cc(c(cc12)OCC1C[C@H]2[C@H](CN(C2)C)C1)OC)Nc1c(c(c(cc1)Cl)Cl)F
Chemical Structure

Biological activities

XL647 is a novel spectrum-selective, reversible and ATP competitive kinase inhibitor. XL647 possesses potent inhibitory activity against the EGF and vascular endothelial growth factor receptor tyrosine kinase families, both wild-type (WT) and mutant vascular endothelial growth factor receptor tyrosine kinase families (EGFR).The IC50 of XL647 is 0.3, 16, and 1.5 nM against EGFR, ErbB2 and KDR, respectively. In contrast, XL647 inhibits Flt-4 and EphB4 with IC50 of 8.7 and 1.4 nM, respectively.^[1] In vitro, XL647 inhibits wild type EGFR phosphorylation with an IC50 of 1 nM in squamous cell carcinoma cell line, Lx-1. XL647 inhibits the WT EGFR, with an IC50 value of 12 nM, in pCMV/Lx-1 cells. In A431 cells, XL647 reduces cell viability with an IC50 of 13 nM. Treatment with 10 µM XL647 results in an almost complete inhibition of EGFR, AKT, and ERK phosphorylation. In addition, XL647 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. ^[1] XL647 inhibits the EGFR T790M variant. XL647 also inhibits mutant forms of ErbB2 associated with lapatinib resistance. XL647 inhibits Ba/F3 cell viability with all 17 ErbB2 mutations including E812K and E719G.^[2] XL647 shows potent and long-lived inhibition of the WT EGFR in vivo. XL647 substantially suppresses the growth of H1975 xenograft tumors. XL647 reduces both tumor EGFR signaling and tumor vessel density. Additionally, XL647, in contrast to erlotinib, substantially inhibits the growth and vascularization of MDA-MB-231 xenografts.^[1]

Protocols

EXEL-7647 is formulated for oral administration by dissolution of the dry powder in sterile filtered ( 0.45 µm) saline ( 0.9%) or in sterile water for injection.^[1]

References

[1] Gendreau SB, et al. Inhibition of the T790M gatekeeper mutant of the epidermal growth factor receptor by EXEL-7647. Clin Cancer Res. 2007, 13(12): 3713-3723. [2] Trowe T, et al. EXEL-7647 inhibits mutant forms of ErbB2 associated with lapatinib resistance and neoplastic transformation. Clin Cancer Res. 2008, 14(8): 2465-2475.

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