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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Description: BI-1347 is a novel, potent and selective CDK8 inhibitor with an IC50 of 1.1 nM. Compound I-003 from patent WO2017202719A1
Targets |
CDK8 (IC50 = 1.1 nM)
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ln Vitro |
BI-1347 (150 nM; 44 h) increases the production of granzyme B (GZMB+) in mouse splenic NK cells[2].
BI-1347 (0.1 nM-10 μM; 24 h) treatment causes NK92MI cells to secrete more perforin[2]. |
ln Vivo |
BI-1347 (oral gavage; 10 mg/kg; once daily; 30 d) exhibits anti-tumor activity and modulates STAT1S727 phosphorylation in vivo[2]. In the mammary carcinoma EMT6 model, the combination of BI-1347 intermittent schedule and BI-8382 continuous treatment increases efficacy compared to each monotherapy[2].
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Cell Assay |
Cell Line: Mouse splenic NK cells
Concentration: 150 nM Incubation Time: 44 hours Result: Increased the proportion of granzyme B-positive NK cells by approximately 4-fold. |
Animal Protocol |
B16-F10-luc2 syngeneic melanoma model[2]
10 mg/kg Oral gavage; 10 mg/kg; once daily; 30 d |
References |
Molecular Formula |
C22H20N4O
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Molecular Weight |
356.420404434204
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Exact Mass |
356.16
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Elemental Analysis |
C, 74.14; H, 5.66; N, 15.72; O, 4.49
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CAS # |
2163056-91-3
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Related CAS # |
2163056-91-3
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Appearance |
Solid powder
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SMILES |
CN(C)C(=O)CN1C=C(C=N1)C2=CC=C(C=C2)C3=CN=CC4=CC=CC=C43
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InChi Key |
WULUGQONDYDNKY-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H20N4O/c1-25(2)22(27)15-26-14-19(12-24-26)16-7-9-17(10-8-16)21-13-23-11-18-5-3-4-6-20(18)21/h3-14H,15H2,1-2H3
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Chemical Name |
2-[4-(4-isoquinolin-4-ylphenyl)pyrazol-1-yl]-N,N-dimethylacetamide
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Synonyms |
BI-1347; BI1347; BI 1347
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HS Tariff Code |
2934.99.03.00
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 71~125 mg/mL (199.2~350.7 mM)
Ethanol: ~11 mg/mL (~30.9 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8057 mL | 14.0284 mL | 28.0568 mL | |
5 mM | 0.5611 mL | 2.8057 mL | 5.6114 mL | |
10 mM | 0.2806 mL | 1.4028 mL | 2.8057 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Lysis of B-chronic lymphocytic leukemia cells in presence of Rituximab and the CDK8/19 inhibitor BI-1347. Mol Cancer Ther . 2020 Apr;19(4):1018-1030. td> |
The SMAC mimetic BI-8382 enhances CDK8/19 inhibitor (BI-1347)-mediated NK cell tumor lysis and survival in the EMT6 murine breast cancer model (8–10 mice per group). Mol Cancer Ther . 2020 Apr;19(4):1018-1030. td> |