SKU:K1371 | M. Wt:482.62 | ||
Formula:C30H34N4O2 | Solubility:No | ||
Purity:>99% | Storage:2 years at -20 degrees centigrade | ||
CAS No.:1256580-46-7 | Synonyms:N/A | ||
Chemical NameN/A |
供货周期: | 一周 |
品牌: | |
规格: | 2mg |
货号: | K1371 |
CAS号: | 1256580-46-7 |
SKU:K1371 | M. Wt:482.62 | ||
Formula:C30H34N4O2 | Solubility:No | ||
Purity:>99% | Storage:2 years at -20 degrees centigrade | ||
CAS No.:1256580-46-7 | Synonyms:N/A | ||
Chemical NameN/A |
Description | CH5424802 | |||||
---|---|---|---|---|---|---|
Targets | ALK | |||||
IC50 | 1.9 nM | |||||
In vitro | 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-H522 cells (EGFR wild-type, KRAS wild-type, and ALK wild-type) in monolayer culture. | |||||
In vivo | The half-life and the oral bioavailability of CH5424802 in mice are 8.6 hours and 70.8%, respectively. At a repeated dose of 6 mg/kg, the mean plasma levels reached 1.7, 1.5, and 0.3 nM at 2, 7, and 24 hours post-dose, respectively. Administration of CH5424802 leads to tumor growth prevention and tumor regression. Tumor growth inhibition at 20 mg/kg is 119% for KARPAS-299 and 104% for NB-1 on day 20. CH5424802 inhibits the phosphorylation of STAT3 in a dose-dependent manner (20 mg/kg). | |||||
Clinical Trials | N/A | |||||
Features | N/A |
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