1. MAPK/ERK Pathway
  2. Raf
  3. BI-882370

BI-882370 

目录号: HY-107779 纯度: 99.16%
产品使用指南

BI-882370 是一种高效选择性的 RAF 激酶抑制剂,其结合位于 BRAF 激酶的 DFG-out 无活性构象处 (ATP 结合位点)。 BI-882370 抑制 BRAFV600E-mutant, WT BRAF 和 CRAF 激酶的 IC50 值分别为 0.4,0.8 和 0.6 nM。BI-882370 也可以抑制 SRC 家族激酶。

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BI-882370 Chemical Structure

BI-882370 Chemical Structure

CAS No. : 1392429-79-6

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生物活性

BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases[1].

IC50 & Target[1]

Braf

0.6 nM (IC50)

c-Raf

0.8 nM (IC50)

BRafV600E

0.4 nM (IC50)

体外研究
(In Vitro)

BI-882370 (0.9-6000 nM; 3 days) inhibits the BRAF-mutant human melanoma and colorectal cancer cells proliferation with a EC50 range of 1-10 nM[1].
BI 882370 (0.1-100 nM, 0.1-3000 nM; 2 hours) results in a reduction of p-MEK1/2, p-ERK1/2 and cyclin D1/D2 expression in BRAFV600E-mutant A375 cells; induces phosphorylation of MEK1/2 and enhanced phosphorylation of ERK1/2 in WT BRO cells (3-300 nM)[1].
BI 882370 (0.1-100 nM, 0.1-3000 nM; 24 hours) suppresses cyclin D1/D2 expression, induces Kip1/p27 expression at concentrations of 1 nM or higher in BRAFV600E-mutant A375 cells, expression of cyclins D1/D2 or Kip1/p27 is not affected in WT BRO cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: BRAF-mutant and WT melanoma cell lines (A101D, A375, SK-MEL-28, G-361, and BRO); Colorectal cancer cell lines (COLO 205, HT-29, LS411N, and HCT-116)
Concentration: 0.9-6000 nM
Incubation Time: 3 days
Result: Showed a EC50 range of 1-10 nM in an extended panel of BRAF-mutant human melanoma and colorectal cancer cell; while proliferation of BRAF WT cells was inhibited with EC50 >1 μM.

Western Blot Analysis[1]

Cell Line: BRAFV600E-mutant A375 cells; BRAF WT, NRAS-mutant BRO (WT BRO) cells
Concentration: 0.1-100 nM; 0.1-3000 nM
Incubation Time: 2 hours; 24 hours
Result: Resulted in a reduction of phospho-MEK1/2 signals and cyclin D1/D2 expression in BRAFV600E-mutant A375 cells.
体内研究
(In Vivo)

BI-882370 (deliver orally; 25 mg/kg, 50 mg/kg; twice daily; 2 weeks) is efficacious in multiple mouse models of BRAF-mutant melanomas and colorectal carcinomas, shows superior efficacy compared with Vemurafenib, Dabrafenib, or Trametinib[1].
BI-882370 (deliver orally; 25 mg/kg; twice daily; 40 days) developes resistance within 3 weeks, but resistance is not observed during 5 weeks of second-line therapy in combination with trametinib[1].
BI-882370 (deliver orally; 60 mg/kg; once daily; 2 weeks) indicates lack of toxicity in terms of clinical chemistry, hematology, pathology, and toxicogenomics in rats[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Human melanoma xenografts in nude mice with BRAF-mutant melanomas and colorectal carcinomas cells (A375, COLO 205; G-361, HT-29 cells)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: Deliver orally; 25 mg/kg, 50 mg/kg; twice daily; 2 weeks
Result: Regressed tumors partially, upon discontinuation, tumor regrowth was markedly delayed.
分子量

569.67

Formula

C28H33F2N7O2S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (8.78 mM; ultrasonic and warming and heat to 60°C)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7554 mL 8.7770 mL 17.5540 mL
5 mM 0.3511 mL 1.7554 mL 3.5108 mL
10 mM --- --- ---
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献

纯度: 99.16%

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产品名称:
BI-882370
目录号:
HY-107779
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