BI-882370, inhibitor
BI-882370
Purity
98.00%
Synonyms
BI-882370; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: Soluble
(<1mg/ refers to the product slightly soluble or insoluble)
(<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.
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Related Product Information for BI-882370, inhibitor
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.
References
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.
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Product Notes
The BI-882370 (Catalog #AAA5764306) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "BI-882370, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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