BI-847325

BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively.

Product information

CAS Number: 1207293-36-4

Molecular Weight: 464.56

Formula: C29H28N4O2

Chemical Name: 3-[(3Z)-3-[({4-[(dimethylamino)methyl]phenyl}amino)(phenyl)methylidene]-2-oxo-2,3-dihydro-1H-indol-6-yl]-N-ethylprop-2-ynamide

Smiles: CCNC(=O)C#CC1C=C2NC(=O)/C(=C(\NC3C=CC(CN(C)C)=CC=3)/C3C=CC=CC=3)/C2=CC=1

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-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 16.67 mg/mL (35.88 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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.

Products are for research use only. Not for human use.