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BI-847325

CAT: 0013-GTR19164306-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19164306-01Size:200 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
A novel ATP-competitive MEK/Aurora kinase inhibitor; inhibts human Aurora A (IC50=25 nM) and Aurora C (IC50=16 nM) ; also inhibits MEK1 (IC50=25 nM) and MEK2 (IC50=6 nM) ; reduces expression of p-ERK and p-Histone 3 in multiple models of vemurafenib resistance; decreases the expression of MEK and Mcl-1 and increases the expression of BIM; orally bioavailable.Solid Tumors Phase 1 Clinical (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.
CAS Number
1207293-36-4
Product Name Alternative
BI847325 | BI 847325
Purity
>98% (HPLC)
Solubility
DMSO: ≥36 mg/mL
Smiles
O=C (NCC) C#CC1=CC (NC/2=O) =C (C=C1) C2=C (NC3=CC=C (CN (C) C) C=C3) /C4=CC=CC=C4
Molecular Formula
C29H28N4O2
Molecular Weight
464.5582
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
2-Propynamide, 3-[3-[[[4-[ (dimethylamino) methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-6-yl]-N-ethyl-

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