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BI-882370

Catalog No. TQ0048 CAS 1392429-79-6

BI-882370 is a specific RAF kinase inhibitor. BI-882370 inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases (IC50s: 0.4, 0.8 and 0.6 nM). BI-882370 also inhibits SRC family kinases.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

BI-882370, CAS 1392429-79-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 52.00
5 mg	In stock	$ 77.00
10 mg	In stock	$ 137.00
25 mg	In stock	$ 247.00
50 mg	In stock	$ 445.00

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Purity: 99.07%

Purity: 97.33%

Biological Description

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Storage & Solubility Information

Description	BI-882370 is a specific RAF kinase inhibitor. BI-882370 inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases (IC50s: 0.4, 0.8 and 0.6 nM). BI-882370 also inhibits SRC family kinases.
Targets&IC50	B-Raf (V600E):0.4 nM, B-Raf:0.6 nM, C-Raf:0.8 nM
In vitro	BI-882370 (0.9-6000 nM; 3 days) inhibits the BRAF-mutant human melanoma and colorectal cancer cell proliferation (EC50: 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 BRAFV600E-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 BRAFV600E-mutant A375 cells, expression of cyclins D1/D2 or Kip1/p27 is not affected in WT BRO cells.
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 show superior efficacy compared with Vemurafenib, Dabrafenib, or Trametinib. BI-882370 (p.o; 25 mg/kg; twice daily; 40 days) develops 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) show a lack of toxicity in terms of clinical chemistry, hematology, pathology, and toxicogenomics in rats.
Cell Research	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
Animal Research	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

Molecular Weight	569.67
Formula	C28H33F2N7O2S
CAS No.	1392429-79-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5 mg/mL (8.78 mM), Sonification and heating to 60℃ are recommended.

References and Literature

1. Waizenegger IC, et al. A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation. Mol Cancer Ther. 2016 Mar;15(3):354-65.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Inhibitor Library Anti-Colorectal Cancer Compound Library MAPK Inhibitor Library Anti-Prostate Cancer Compound Library Anti-Cancer Compound Library Anti-Pancreatic Cancer Compound Library Kinase Inhibitor Library Bioactive Compounds Library Max

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Keywords

BI-882370 1392429-79-6 MAPK Raf inhibit Inhibitor Raf kinases BI882370 BI 882370 inhibitor

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