CH5424802 Inhibitor CAS No. 1256580-46-7

Cat. No.	Name	Size	Price
KI0646	CH5424802	5 mg	$272
	CH5424802	10 mg	$432
	CH5424802	50 mg	$1232
	CH5424802	100 mg	$2032

Chemical Characteristic

Product Name	CH5424802
Synonyms	AF802,Alectinib
CAS No.	1256580-46-7
Molecular Weight	482.62
Formula	C₃₀H₃₄N₄O₂
Chemical Structure

Biological activities

CH5424802 is a potent, selective and orally available anaplastic lymphoma kinase (ALK) inhibitor. In cell-free assays, CH5424802 inhibits the enzyme activity of ALK, ALK^F1174L and ALK^R1275Q with IC50 of 1.9, 1.0 and 3.5 nM, respectively. CH5424802 has substantial inhibitory potency against both native ALK and L1196M with Ki of 0.83 and 1.56 nM, respectively. In cellular phosphorylation assays, CH5424802 can prevent autophosphorylation of ALK in NCI-H2228 NSCLC cells expressing EML4-ALK. CH5424802 suppresses the phosphorylation of STAT3 in a dose-dependent manner (2閳?0 mg/kg). In the NCI-H2228 model, once-daily oral administration of CH5424802 results in dose-dependent tumor growth inhibition with an ED50 of 0.46 mg/kg and tumor regression. Administration of CH5424802 leads to significant tumor regression against both native EML4-ALK- and L1196M-driven tumors.^[1] In the Ba/F3-EML4-ALK^L1196M bearing xenograft study, a dosage of 60 mg/kg of CH5424802 decreases the tumor sizes after 8 days of treatment. ^[2]

References

[1] Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5): 679-690. 閵嗏偓閵嗏偓 [2] Shiao HY, et al. Anaplastic Lymphoma Kinase (ALK) Inhibitors: New Cancer Breakthroughs for Lung Cancer. The Chinese Oncology Society. 2011. 閵嗏偓閵嗏偓

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