CH5424802 Hydrochloride_1256589-74-8_DataSheet_MedChemExpress

Product Name:

CH5424802 Hydrochloride CAS No.:

1256589-74-8Cat. No.:

HY-13011A MWt:

519.08Formula:

C30H35ClN4O2Purity :>98%

Solubility:

Mechanisms:

Biological Activity:

References:

Caution: Not fully tested. For research purposes only

Medchemexpress LLC

https://www.wendangku.net/doc/8617250657.html,

[1]. Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper

mutant. Cancer Cell. 2011, 19(5), 679-690.[2]. Kinoshita K, et al. Design and synthesis of a highly selective, orally active and potent anaplastic

lymphoma kinase inhibitor (CH5424802). Bioorg Med Chem. 2012, 20(3), 1271-1280.CH5424802 Hcl (AF 802 Hcl; Alectinib Hcl) is a potent ALK inhibitor with IC50 of 1.9 nM, sensitive to L1196M

mutation.

IC50 value: 1.9 nM [1]

Target: ALK in vitro: The dissociation constant (KD) value of CH5424802 for ALK in an ATP-competitive manner is 2.4nM. CH5424802 has substantial inhibitory potency against both native ALK and L1196M with Ki of 0.83 nM and 1.56 nM, respectively. CH5424802 prevents autophosphorylation of ALK in NCI-H2228 NSCLC cells expressing EML4-ALK. CH5424802 also suppresses the phosphorylation of STAT3 and AKT, but not of ERK1/2. CH5424802 completely inhibits the phosphorylation of STAT3 at Tyr705. CH5424802 is

preferentially efficacious against NCI-H2228 cells expressing EML4-ALK, but not ALK fusion-negative

NSCLC cell lines, including HCC827 cells (EGFR exon 19 deletion), A549 cells (KRAS mutant), or NCI-H522cells (EGFR wild-type, KRAS ...

Pathways:Protein Tyrosine Kinase/RTK; Target:ALK

Product Data Sheet

11 D e e r P a r k D r i v e , S u i t e 102D M o n m o u t h J u n c t i o n , N J 08852,U S A

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