Zeteletinib

Name: Zeteletinib
Brand: TargetMol
SKU: T39688
Price: 440 USD
Availability: InStock
Rating: 4.5 (1 reviews)

很棒

产品编号 T39688Cas号 2216753-97-6

别名 Zeteletinib, DS-5010, BOS-172738

Zeteletinib (BOS-172738; DS-5010) is a highly potent and selective orally active inhibitor of the RET kinase. It demonstrates nanomolar potency against RET while exhibiting over 300-fold selectivity against VEGFR2. Zeteletinib exhibits remarkable efficacy against the wild-type RET, RET V804M/L gatekeeper mutants, as well as the frequently occurring oncogenic RET mutation M918T. Its antitumor activity is potent.

Zeteletinib

很棒

产品编号 T39688 别名 Zeteletinib, DS-5010, BOS-172738Cas号 2216753-97-6

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产品介绍

生物活性

产品描述	Zeteletinib (BOS-172738; DS-5010) is a highly potent and selective orally active inhibitor of the RET kinase. It demonstrates nanomolar potency against RET while exhibiting over 300-fold selectivity against VEGFR2. Zeteletinib exhibits remarkable efficacy against the wild-type RET, RET V804M/L gatekeeper mutants, as well as the frequently occurring oncogenic RET mutation M918T. Its antitumor activity is potent.
体外活性	In biochemical assays of 106 kinases, RET and platelet-derived growth factor receptor (PDGFR) alpha/beta were inhibited more than 80% by 193 nM Zeteletinib (BOS-172738; DS-5010). The IC 50 values of Zeteletinib against RET, RET-GKm (V804L) were single digit nano-molar even under a condition of high concentration of ATP; besides it against KDR was more than 1000 nM[1].
体内活性	In a Ba/F3-RET subcutaneous tumor model, Zeteletinib (BOS-172738; DS-5010) dosing at 10 mg/kg twice daily (bid) induces tumor regression[1]. In an LC2/ad NSCLC xenograft model, which has the RET-CCDC6 fusion gene, Zeteletinib dosing at 1 mg/kg thrice daily (tid) induced tumor regression[1].
别名	Zeteletinib, DS-5010, BOS-172738