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CAS No.: 2097132-94-8

Pralsetinib/普拉替尼 Catalog No. CSN22922

Synonyms: BLU-667;普拉替尼

Blu667 is a highly potent and selective RET inhibitor with IC50 value of 0.4nM.

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技术信息

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... more >>g Cancer Medullary Thyroid Cancer RET-altered Papillary Thyroid Cancer RET-altered Colon Cancer RET-altered Solid Tumors Collapse <<	Phase 1	Recruiting	March 2023	-

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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8741 mL
- 9.3703 mL
- 18.7406 mL
- 5 mM
- 0.3748 mL
- 1.8741 mL
- 3.7481 mL
- 10 mM
- 0.1874 mL
- 0.9370 mL
- 1.8741 mL

技术信息

CAS号

2097132-94-8

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H32FN9O2

运输

蓝冰

分子量

533.60

别名

BLU-667;普拉替尼

溶解度

DMSO	175.0 mg/mL (328.0 mM)
Water	insoluble

动物实验配方

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