| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
CMPD 7 (also known as AZ1992) is a novel, highly potent and selective CDK12 inhibitor with an IC50 of 491 nM in an enzymatic assay. AZ1992 is a highly potent and selective CDK12 inhibitor with IC50 = 491 nM. AZ1992 showed 5-fold CDK2 and near 20-fold CDK9 selectivity. AZ1992 was profiled across a panel of 352 kinases at 0.1 mm followed by concentration–response testing in 30 of the top hits, showing that AZ1992 is a highly selective CDK12 inhibitor, and this result was confirmed by affinity proteomics using a kinase affinity matrix.
| ln Vitro |
CDK12-IN-3 is a CDK12 reagent that is very sensitive. Strong suppression of Ser2 phosphorylation on RNA Pol II's CTD repeat domain, together with OV90 cell growth inhibition and THP1 cell acute cytotoxicity, are demonstrated by CDK12-IN-3 (0.1 μM) [1].
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|---|---|
| References |
| Molecular Formula |
C23H28F2N8O
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|---|---|
| Molecular Weight |
470.518230438232
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| Exact Mass |
470.235
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| CAS # |
2220184-50-7
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| Appearance |
White to off-white solid powder
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| LogP |
3.4
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| SMILES |
FC1=C(C=CC2=C1N=C(CNC1C3=C(N(C=N3)C(C)C)N=C(N=1)N1CCCCC1CCO)N2)F
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| InChi Key |
KULPPFCRBINTBS-AWEZNQCLSA-N
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| InChi Code |
InChI=1S/C23H28F2N8O/c1-13(2)33-12-27-20-21(26-11-17-28-16-7-6-15(24)18(25)19(16)29-17)30-23(31-22(20)33)32-9-4-3-5-14(32)8-10-34/h6-7,12-14,34H,3-5,8-11H2,1-2H3,(H,28,29)(H,26,30,31)/t14-/m0/s1
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| Chemical Name |
(S)-2-(1-(6-(((6,7-Difluoro-1H-benzo[d]imidazol-2-yl)methyl)amino)-9-isopropyl-9H-purin-2-yl)piperidin-2-yl)ethan-1-ol
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| Synonyms |
CMPD7;CMPD 7; CMPD-7; AZ1992; AZ-1992; AZ 1992; Compound 7
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| HS Tariff Code |
2934.99.9001
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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 : ~250 mg/mL (~531.33 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.33 mg/mL (4.95 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 23.3 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: ≥ 2.33 mg/mL (4.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 23.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1253 mL | 10.6265 mL | 21.2531 mL | |
| 5 mM | 0.4251 mL | 2.1253 mL | 4.2506 mL | |
| 10 mM | 0.2125 mL | 1.0627 mL | 2.1253 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.
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