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商品描述
BI-847325
- Catalog No.：MC0928
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo：
- 1207293-36-4
- MolecularFormula：
- C29H28N4O2
- Purity：
- >98%
- Target：
- MEK
- IC50：
- IC50: 25 nM (hAK-A), 15 nM (hAK-C), 25 nM (MEK1), 4 nM (MEK2)[1]
- In Vitro：
- BI 847325 inhibits the activity of X. laevis AK-B with an IC50 of 3 nM; the IC50 values for human AK-A and AK-C are 25 and 15 nM, respectively. BI 847325 also inhibits human MEK1 and MEK2 with respective IC50 values of 25 and 4 nM. BI 847325 at 1,000 nM inhibits 6 enzymes by more than 50% (LCK, MAP3K8, FGFR1, AMPK, CAMK1D and TBK1) and the IC50 values are below 100 nM only for LCK (5 nM) and MAP3K8 (93 nM). Proliferation is inhibited in A375 and Calu-6 cell lines with GI50 values of 7.5 nM and 60 nM, respectively[1].
- In Vivo：
- Daily oral administration of BI 847325 at 10 mg/kg shows efficacy in both BRAF- and KRAS-mutant xenograft models. BI 847325 administered once weekly at 70 mg/kg inhibits both MEK and AK in KRAS-mutant tumors[1].
- Fields：
- BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
- Specificity：
- Target: MEK. Fields: BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A an
- Source：
- Rabbit
- Dilution：
- IC50: 25 nM (hAK-A), 15 nM (hAK-C), 25 nM (MEK1), 4 nM (MEK2)[1]
- Concentration：
- >98%
- Storage Stability：
- 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
- Other Name：
- BI-847325,BI 847325,BI847325
- MolecularWeight(Da)：
- 464.56
- References：
- [1]. Sini P, et al. Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases. Mol Cancer Ther. 2016 Oct;15(10):2388-2398.
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