BI-882370|cas:1392429-79-6|西域试剂

BI-882370,99.16%

产品编号：Bellancom-107779| CAS NO：1392429-79-6| 分子式：C₂₈H₃₃F₂N₇O₂S| 分子量：569.67

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货号	价格	库存与货期
Bellancom-107779	￥950.00	杭州北京（现货）
Bellancom-107779	￥1700.00	杭州北京（现货）
Bellancom-107779	￥5500.00	杭州北京（现货）
Bellancom-107779	￥9700.00	杭州北京（现货）

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BI-882370

产品介绍

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 BRAF^V600E-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。

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 BRAF^V600E-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.

体外研究

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.
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 BRAF^V600E-mutant A375 cells; induces phosphorylation of MEK1/2 and enhanced phosphorylation of ERK1/2 in WT BRO cells (3-300 nM).
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 BRAF^V600E-mutant A375 cells, expression of cyclins D1/D2 or Kip1/p27 is not affected in WT BRO cells.

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

Cell Proliferation Assay

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

Cell Line:	BRAF^V600E-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 BRAF^V600E-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.
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.
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.

西域 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)
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.

体内研究

西域 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)
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.

体内研究

西域 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)
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.

性状

Solid

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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式