BI-847325
- CAS No.
- 1207293-36-4
- Chemical Name:
- BI-847325
- Synonyms
- BI-847325;BI 847325;BI847325;BI-847325, 10 mM in DMSO;BI-847325;BI 847325;BI847325;BI-847325, 98%, an ATP competitive dual inhibitor of MEK and aurora kinases (AK);3-[3-[[4-(dimethylaminomethyl)anilino]-phenylmethylidene]-2-oxo-1H-indol-6-yl]-N-ethylprop-2-ynamide;3-(3-(((4-((Dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide;(Z)-3-(3-(((4-((Dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide;3-[3-[[[4-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-6-yl]-N-ethyl-2-propynamide;2-Propynamide, 3-[3-[[[4-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-6-yl]-N-ethyl-
- CBNumber:
- CB12743902
- Molecular Formula:
- C29H28N4O2
- Molecular Weight:
- 464.56
- MDL Number:
- MFCD28978743
- MOL File:
- 1207293-36-4.mol
- MSDS File:
- SDS
| storage temp. | Store at -20°C |
|---|---|
| solubility | ≥24.1 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| form | crystalline solid |
| color | Light yellow to yellow |
| FDA UNII | QXD8ZW7UVZ |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P305+P351+P338 | |||||||||
| NFPA 704 |
|
BI-847325 price More Price(23)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 18301 | BI-847325 ≥98% | 1207293-36-4 | 1mg | $73 | 2024-03-01 | Buy |
| Cayman Chemical | 18301 | BI-847325 ≥98% | 1207293-36-4 | 5mg | $171 | 2024-03-01 | Buy |
| TRC | B591715 | BI-847325 | 1207293-36-4 | 100mg | $1240 | 2021-12-16 | Buy |
| ApexBio Technology | B6014 | BI-847325 | 1207293-36-4 | 5mg | $173 | 2021-12-16 | Buy |
| AK Scientific | 3237EM | 3-[3-[N-[4-[(Dimethylamino)methyl]phenyl]-C-phenylcarbonimidoyl]-2-hydroxy-1H-indol-6-yl]-N-ethylprop-2-ynamide | 1207293-36-4 | 1mg | $179 | 2021-12-16 | Buy |
BI-847325 Chemical Properties,Uses,Production
Description
BI-847325 is a selective dual MEK/Aurora kinase inhibitor with IC50 values of 3, 25, 15, 25, and 4 nM for X. laevis Aurora B, human Aurora A and Aurora C, and human MEK1 and MEK2, respectively. It can inhibit the growth and survival of both treatment-naive and drug-resistant melanoma cell lines, decreasing the expression of MEK and Mcl-1 while increasing the expression of pro-apoptotic protein Bim. At 70 mg/kg, BI-847325 induces apoptosis in treatment-naive and drug-resistant xenografted melanoma in vivo.
Uses
BI-847325 is a novel ATP-competitive MEK and Aurora kinase inhibitor. It can inhibit the growth of BRAF resistant melanoma cells through suppression of Mcl-1 and MEK expression in human melanoma cell lines and mouse xenograft model. The efficacy of BI-847325 was studied in patients with refractory solid tumors.
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].
IC 50
MEK2: 4 nM (IC50); Aurora C: 15 nM (IC50)
References
[1]. sini p, gürtler u, zahn sk, et al. pharmacological characterization of bi 847325, a dual inhibitor of mek and aurora kinases. cancer research, 2012, 72(8 supplement): 1919-1919.
[2]. hideshima t, chauhan d, richardson p, et al. nf-κb as a therapeutic target in multiple myeloma. journal of biological chemistry, 2002, 277(19): 16639-16647.
[3]. rommel c, clarke ba, zimmermann s, et al. differentiation stage-specific inhibition of the raf-mek-erk pathway by akt. science, 1999, 286(5445): 1738-1741..
BI-847325 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19552 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32268 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30230 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| Finetech Industry Limited | +86-27-8746-5837 +8619945049750 | info@finetechnology-ind.com | China | 9642 | 58 |
| Hefei Hirisun Pharmatech Co., Ltd | +8615056975894 | shawn@hirisunpharm.com | CHINA | 9911 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38663 | 58 |
