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BI-882370

Katalog-Nr.GC18178

BI-882370 ist ein potenter und selektiver RAF-Kinase-Inhibitor, der an die ATP-Bindungsstelle der Kinase bindet, die in der DFG-out- (inaktiven) Konformation der BRAF-Kinase positioniert ist. BI-882370 (BI 882370) hemmt die onkogene BRAFV600E-Mutante, die WT-BRAF- und CRAF-Kinasen mit IC50-Werten von 0,4, 0,8 bzw. 0,6 nM. BI-882370 hemmt auch Kinasen der SRC-Familie.

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BI-882370 Chemische Struktur

Cas No.: 1392429-79-6

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Sample solution is provided at 25 µL, 10mM.

Product Documents

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Background

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].

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].

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].

References:
[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.

Chemical Properties

Cas No. 1392429-79-6 SDF
Chemical Name N-[3-[5-[(1-ethyl-4-piperidinyl)methylamino]-3-(5-pyrimidinyl)-1H-pyrrolo[3,2-b]pyridin-1-yl]-2,4-difluorophenyl]-1-propanesulfonamide
Canonical SMILES CCN1CCC(N(C)C2=CC=C(N(C3=C(F)C=CC(NS(CCC)(=O)=O)=C3F)C=C4C5=CN=CN=C5)C4=N2)CC1
Formula C28H33F2N7O2S M.Wt 569.7
Löslichkeit DMF: 100µ g/ml,DMSO: 100µ g/ml,Ethanol: 100µ g/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.7553 mL 8.7765 mL 17.5531 mL
5 mM 0.3511 mL 1.7553 mL 3.5106 mL
10 mM 0.1755 mL 0.8777 mL 1.7553 mL
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