- BI-1347
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- $34.00
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2026-04-22
- CAS:2163056-91-3
- Purity: 99.63%
- Supply Ability: 10g
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| 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 | | EINECS: | | | Product Categories: | | | Mol File: | 2163056-91-3.mol |  |
| 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 |
| 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 |
| | None Preparation Products And Raw materials |
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