BI-847325 - CAS 1207293-36-4
Catalog number: B0084-470824
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C29H28N4O2
Molecular Weight:
464.56
COA:
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Targets:
Aurora Kinase | MEK
Description:
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.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-470824 10 mg $169 In stock
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Purity:
98%
Appearance:
Solid Powder
Synonyms:
BI-847325; BI 847325; BI847325.
Solubility:
DMSO: 19mg/mL warmed(40.89mM); Ethanol: 1mg/mL(2.15mM); Water: <1mg/mL(<1mM)
Storage:
3 years -20℃ powder; 6 months -80℃ in solvent
MSDS:
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Shelf Life:
2 years
InChIKey:
FLBNLJLONKAPLR-DQSJHHFOSA-N
InChI:
InChI=1S/C29H28N4O2/c1-4-30-26(34)17-13-20-12-16-24-25(18-20)32-29(35)27(24)28(22-8-6-5-7-9-22)31-23-14-10-21(11-15-23)19-33(2)3/h5-12,14-16,18,31H,4,19H2,1-3H3,(H,30,34)(H,32,35)/b28-27-
Canonical SMILES:
CCNC(=O)C#CC1=CC2=C(C=C1)C(=C(C3=CC=CC=C3)NC4=CC=C(C=C4)CN(C)C)C(=O)N2
1.The Novel ATP-Competitive MEK/Aurora Kinase Inhibitor BI-847325 Overcomes Acquired BRAF Inhibitor Resistance through Suppression of Mcl-1 and MEK Expression.
Phadke MS;Sini P;Smalley KS Mol Cancer Ther. 2015 Jun;14(6):1354-64. doi: 10.1158/1535-7163.MCT-14-0832. Epub 2015 Apr 14.
Resistance to BRAF inhibitors is a major clinical problem. Here, we evaluate BI-847325, an ATP-competitive inhibitor of MEK and Aurora kinases, in treatment-naïve and drug-resistant BRAF-mutant melanoma models. BI-847325 potently inhibited growth and survival of melanoma cell lines that were both BRAF inhibitor naïve and resistant in 2D culture, 3D cell culture conditions, and in colony formation assays. Western blot studies showed BI-847325 to reduce expression of phospho-ERK and phospho-histone 3 in multiple models of vemurafenib resistance. Mechanistically, BI-847325 decreased the expression of MEK and Mcl-1 while increasing the expression of the proapoptotic protein BIM. Strong suppression of MEK expression was observed after 48 hours of treatment, with no recovery following >72 hours of washout. siRNA-mediated knockdown of Mcl-1 enhanced the effects of BI-847325, whereas Mcl-1 overexpression reversed this in both 2D cell culture and 3D spheroid melanoma models. In vivo, once weekly BI-847325 (70 mg/kg) led to durable regression of BRAF-inhibitor naïve xenografts with no regrowth seen (>65 days of treatment). In contrast, treatment with the vemurafenib analog PLX4720 was associated with tumor relapse at >30 days.
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CAS 1207293-36-4 BI-847325

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