None
None Basic information
- Product Name:
- None
- Synonyms:
-
- BI-1347 (BI1347)
- 1H-Pyrazole-1-acetamide, 4-[4-(4-isoquinolinyl)phenyl]-N,N-dimethyl-
- 2-(4-(4-(Isoquinolin-4-yl)phenyl)-1H-pyrazol-1-yl)-N,N-dimethylacetamide
- BI-1347,None,2-{4-[4-(isoquinolin-4-yl)phenyl]-1H-pyrazol-1-yl}-N,N-dimethylacetamide
- BI1347,oral activity,human NK92MI cell,BI-1347,Inhibitor,CDK,mouse splenic NK cell,BI 1347,anti-tumoral activity,inhibit,Cyclin dependent kinase,selectivity
- BI-1347, 10 mM in DMSO
- B1-1347
- CAS:
- 2163056-91-3
- MF:
- C22H20N4O
- MW:
- 356.42
- Mol File:
- 2163056-91-3.mol
None Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO:98.0(Max Conc. mg/mL);274.95(Max Conc. mM)
Ethanol:3.0(Max Conc. mg/mL);8.42(Max Conc. mM) - form
- Solid
- color
- Light yellow to yellow
None Usage And Synthesis
Uses
BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity[1][2].
in vivo
BI-1347 (oral gavage; 10 mg/kg; once daily; 30 d) modulates STAT1 S727 phosphorylation and shows anti-tumor activity in vivo[2].
BI-1347 (oral gavage; 10 mg/kg) intermittent schedule and BI-8382 continuous treatment combination treatment increases efficacy compared to each monotherapy in the mammary carcinoma EMT6 model[2].
| Animal Model: | B16-F10-luc2 syngeneic melanoma model[2] |
| Dosage: | 10 mg/kg |
| Administration: | Oral gavage; 10 mg/kg; once daily; 30 d |
| Result: | Reduced phosphorylation of STAT1 S727 for at least 6 h by 60%. Showed minimal effect on body weight at 10 mg/kg. Showed lower tumor burden both on day 23 and 29, compared to the control group. |
IC 50
CDK8: 1.1 nM (IC50)
References
[1] Harald Engelhardt, et al. New phenylpyrazolylacetamide compounds and derivatives as cdk8/cdk19 inhibitors.
[2] Hofmann MH, et al. Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance. Mol Cancer Ther. 2020 Apr;19(4):1018-1030. DOI:10.1158/1535-7163.MCT-19-0789
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