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BI-882370 Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5764306

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 0.6nM). BI-882370 also inhibits SRC family kinases. More details

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
BI-882370, Inhibitor
Full Product Name
BI-882370
Product Gene Name
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
569.67
Solubility
DMSO: Soluble
(<1mg/ refers to the product slightly soluble or insoluble)
Formula
C28H33F2N7O2S
SMILES
CCCS(Nc(ccc(F)c1-n(cc2-c3cncnc3)c(cc3)c2nc3NCC2CCN(CC)CC2)c1F)(=O)=O
CAS Number
1392429-79-6
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: 0.9-6000nM. Incubation Time: 3 days
In Vitro
BI-882370 (deliver orally; 25mg/kg, 50mg/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; 25mg/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; 60mg/kg; once daily; 2 weeks) show a lack of toxicity in terms of clinical chemistry, hematology, pathology, and toxicogenomics in rats.

Product Categories/Family for BI-882370, inhibitor

Product References and Citations for BI-882370, inhibitor

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.

Other Notes

Small volumes of BI-882370, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for BI-882370 purchase

MBS5764306 is an inhibitor targeting BI-882370.
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