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Chemical Structure| 2097132-94-8 同义名 : BLU-667;CS 3009;Gavreto
CAS号 : 2097132-94-8
货号 : A468588
分子式 : C27H32FN9O2
纯度 : 99%+
分子量 : 533.601
MDL号 : MFCD31810155
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(196.78 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Rearranged during transfection (RET) is a receptor tyrosine kinase that acts as an oncogenic driver in multiple cancers. BLU-667 is a potent, selective, small-molecule RET inhibitor that demonstrates ≥10-fold increased potency over other multi-kinase inhibitors. It inhibited the kinase activity of wild-type RET with an IC50 of 0.4nM. BLU-667 also exhibited potent inhibitory activity against common oncogenic RET alterations, including RET V804L, RET V804M, RET M918T, and CCDC6-RET fusion, with IC50 values of 0.3, 0.4, 0.4, and 0.4nM, respectively. In Ba/F3 cells engineered to express a KIF5B-RET fusion, treatment with BLU-667 inhibited RET autophosphorylation with a cellular IC50 value of 5nM. BLU-667 also inhibited phosphorylation of RET, SHC, and ERK1/2 at concentrations of ≤10nM in RET-driven cell lines. In RET-driven murine models, BLU667 at doses as low as 10mg/kg (twice per day) exhibited concentration-dependent activity against KIF5B-RET Ba/F3 and KIF5B-RET V804L Ba/F3 allograft tumors. BLU-667 at doses of 3 to 60mg/kg also showed potent activity in a RET C634W MTC xenograft, and KIF5B-RET NSCLC and CCDC6-RET CRC patient-derived xenograft models[1].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03037385 RET-altered Non Small Cell Lun... 展开 >>g Cancer Medullary Thyroid Cancer RET-altered Papillary Thyroid Cancer RET-altered Colon Cancer RET-altered Solid Tumors 收起 << Phase 1 Recruiting March 2023 -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.87mL

0.37mL

0.19mL

9.37mL

1.87mL

0.94mL

18.74mL

3.75mL

1.87mL
参考文献

[1]Subbiah V, Gainor JF, Rahal R, et al. Precision Targeted Therapy with BLU-667 for RET-Driven Cancers. Cancer Discov. 2018;8(7):836-849. doi:10.1158/2159-8290.CD-18-0338