| Identification | Back Directory | [Name]
None | [CAS]
2163056-91-3 | [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 | [Molecular Formula]
C22H20N4O | [MDL Number]
MFCD31716761 | [MOL File]
2163056-91-3.mol | [Molecular Weight]
356.42 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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