CAS NO: | 2375837-06-0 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selectiveRETkinaseinhibitor with nanomolar potency againstRETand >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild typeRET,RETV804M/Lgatekeeper mutants, and the most common oncogenicRETmutationM918T. Zeteletinib hemiadipate has potent antitumor activity[1][2][3]. | |
IC50& Target[1] |
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体外研究 (In Vitro) | 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) hemiadipate. The IC50values of Zeteletinib hemiadipate 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]. | |
体内研究 (In Vivo) | 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) hemiadipate. The IC50values of Zeteletinib hemiadipate 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]. | |
Clinical Trial | ||
分子量 | 573.55 | |
Formula | C25H23F3N4O4.1/2C6H10O4 | |
CAS 号 | 2375837-06-0 | |
运输条件 | Room temperature in continental US; may vary elsewhere. | |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |