BLU-667 trans form

• 常用名: BLU-667 trans form
• 英文名: BLU-667 trans form
• CAS号: 2097132-93-7
• 分子量: 533.60
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₇H₃₂FN₉O₂
• 熔点: N/A
• 闪点: N/A

BLU-667 trans form用途

cis-Pralsetinib (cis-Blu667) 是一种 高效选择性的 rearranged during transfection (RET) 抑制剂,抑制野生型 RET 和其四种变异体 (V804L, V804M, M918T, CCDC6-RET) 的 IC50 值为 0.3-0.4 nM。具有广泛的、强有效的抗 RET 驱动的实体瘤活性。

BLU-667 trans form名称

• 英文名: cis-Pralsetinib

BLU-667 trans form生物活性

• 描述: cis-Pralsetinib (cis-Blu667) 是一种 高效选择性的 rearranged during transfection (RET) 抑制剂,抑制野生型 RET 和其四种变异体 (V804L, V804M, M918T, CCDC6-RET) 的 IC50 值为 0.3-0.4 nM。具有广泛的、强有效的抗 RET 驱动的实体瘤活性。
• 相关类别:
  研究领域 >> 癌症
• 靶点实验:

  IC50: 0.4 nM (WT RET), 0.3 nM (RET V804L), 0.4 nM (RET V804M), 0.4 nM (RET M918T), 0.4 nM (CCDC6-RET)[2]

• 参考文献:

  [1]. http://www.blueprintmedicines.com/wp-content/uploads/2017/10/BLU-667-EORTC-2017-BPM.pdf

  [2]. Subbiah V, et al. Precision Targeted Therapy With BLU-667 for RET-Driven Cancers. American Association for Cancer Research. 10.1158/2159-8290.CD-18-0338.

BLU-667 trans form物理化学性质

• 分子式: C₂₇H₃₂FN₉O₂
• 分子量: 533.60
• InChIKey: GBLBJPZSROAGMF-UHFFFAOYSA-N
• SMILES: COC1(C(=O)NC(C)c2ccc(-n3cc(F)cn3)nc2)CCC(c2nc(C)cc(Nc3cc(C)[nH]n3)n2)CC1

BLU-667 trans form靶点实验

查看更多实验

实验名称：Inhibition of KIF5B-RET fusion protein (unknown origin) expressed in mouse BaF3 cells... 来源：ChEMBL 靶标：Proto-oncogene tyrosine-protein kinase receptor Ret External Id：CHEMBL4709982

实验名称：Inhibition of CCDC6-RET fusion protein (unknown origin) expressed in mouse BaF3 cells... 来源：ChEMBL 靶标：Coiled-coil domain-containing protein 6 External Id：CHEMBL4709981

实验名称：Inhibition of KIF5B-RET V804M mutant fusion protein (unknown origin) expressed in mou... 来源：ChEMBL 靶标：Proto-oncogene tyrosine-protein kinase receptor Ret External Id：CHEMBL4709986

实验名称：RET V804L Gatekeeper Mutant Assay at KM from US Patent US10584114: "Inhibitors of RET... 来源：BindingDB 靶标：N/A External Id：BindingDB_8998_3

实验名称：Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation mea... 来源：ChEMBL 靶标：BaF3 External Id：CHEMBL4709987

实验名称：RET Wild Type Assay at KM from US Patent US10584114: "Inhibitors of RET" 来源：BindingDB 靶标：N/A External Id：BindingDB_8998_2

实验名称：Inhibition of CCDC6-RET V804M mutant fusion protein (unknown origin) expressed in mou... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4709985

实验名称：Antiproliferative activity against mouse BaF3 cells expressing rearranged during tran... 来源：ChEMBL 靶标：BaF3 External Id：CHEMBL5250524

实验名称：Antiproliferative activity against mouse BaF3 cells expressing rearranged during tran... 来源：ChEMBL 靶标：BaF3 External Id：CHEMBL5250523

实验名称：Drug level in tumor of mouse transplanted with mouse KIF5B-RET Ba/F3 cells at 10 mg/k... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4836469

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