BLU-285 Avapritinib
- 公司名称 MedChemExpress LLC
- 品牌 MedChemExpress (MCE)
- 型号 BLU-285
- 产地
- 厂商性质 生产厂家
- 更新时间 2019/7/1 18:06:39
- 访问次数 526
联系我们时请说明是化工仪器网上看到的信息,谢谢!
供货周期 | 现货 | 规格 | 10 mM * 1 mL;1 mg;5 mg;10 mg;25 mg;50 mg |
---|---|---|---|
货号 | HY-101561 | 应用领域 | 生物产业 |
Avapritinib
产品活性:Avapritinib 是一种有效的选择性外显子 17 突变型 KIT 激酶抑制剂,抑制 KIT D816V,IC50 为 0.27 nM。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:c-Kit
In Vitro: Avapritinib (BLU-285) has demonstrated biochemical in vitro activity on the KIT exon 17 mutant enzyme, KIT D816V (IC50=0.27 nM). Cellular activity of Avapritinib on KIT D816 mutants is measured by autophosphorylation in the human mast cell leukemia cell line HMC1.2, and the P815 mouse mastocytoma cell line with IC50=4 and 22 nM, respectively. In Kasumi-1 cells, a t(8;21)-positive AML cell line with a KIT exon 17 N822K mutation, Avapritinib potently inhibits KIT N822K mutant autophosphorylation (IC50=40 nM), downstream signaling, as well as cellular proliferation (IC50=75 nM).
In Vivo: In vivo Avapritinib (BLU-285) is well tolerated and has demonstrated dose dependent antitumor efficacy. Complete tumor growth inhibition and ≥75% KIT kinase inhibition is observed with 10 mg/kg once daily, oral dosing of Avapritinib in the aggressive KIT exon 17 mutant driven P815 mastocytoma model grown as a solid tumor allograft as well as in a disseminated model of disease. Disease burden, measured by whole body luciferase imaging (photons/second/mm2), increases 86-fold in the vehicle control animals over the 24 day dosing period with widespread disease detectable in both femurs, the pelvis and circulating in peripheral blood. Avapritinib at both doses (10 or 30 mg/kg orally, once daily) results in a marked reduction of disease burden throughout the study. Avapritinib at either 10 or 30 mg/kg results in tumor regression in all animals with disease abrogation indistinguishable from background signal measurements in several animals by the end of study. Avapritinib is also well tolerated in this in vivo model and has no adverse effects on body weight at either dose.
相关产品:Drug Repurposing Compound Library | Kinase Inhibitor Library | Clinical Compound Library | Clinical Compound Library Plus | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Drug Repurposing Compound Library Plus | Bioactive Compound Library Plus | Pexidartinib | Cabozantinib | Imatinib | Pazopanib | Sitravatinib | Masitinib | Dovitinib | SU14813 | Ripretinib | Motesanib | OSI-930 | AST 487 | c-Kit-IN-1 | Amuvatinib | Flumatinib | Telatinib | AC710 | AZD2932 | PLX647 | AZD3229 | ISCK03