| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
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Purity: ≥98%
CDKI-73 is a novel and potent CDK9 inhibitor with Ki of 4 nM. In comparison to normal B cells and normal CD34+ cells (LD50>20 uM), it demonstrates selective toxicity to CLL cells (LD50=80 nM). Apoptosis is induced and the effects of cisplatin are amplified by CDK9 inhibition.
| Targets |
CDK2 (IC50 = 3.27 nM); CDK9 (IC50 = 5.78 nM); CDK1 (IC50 = 8.17 nM); CDK4 (IC50 = 8.18 nM); CDK6 (IC50 = 37.68 nM); CDK7 (IC50 = 134.26 nM); CDK1 (Ki = 4 nM); CDK2 (Ki = 3 nM); CDK9 (Ki = 4 nM); CDK7 (Ki = 91 nM)
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|---|---|
| ln Vitro |
CDKI-73 primarily targets CDK9 and downregulates the expression of anti-apoptotic proteins Bcl-2, Mcl-1, and XIAP, causing cancer cells to undergo apoptosis. The bone marrow cells of healthy donors, however, are comparatively less toxic to it.[2]
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| ln Vivo |
CDKI-73 targets CDK9 to downregulate anti-apoptotic proteins. It is highly effective against MLL-AML MV4-11 xenografts and is orally bioavailable in vivo.[2]
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| Cell Assay |
MV4-11 (1 × 105/well) cells are seeded and incubated for an entire night at 37ºC with 5% CO2. Cells are gathered and centrifuged (300 g, 5 min) following a 24- or 48-hour incubation period with the indicated concentrations of CDKI-73. The pellets are resuspended in cold 70% ethanol for the cell cycle assay, fixed on ice for 15 minutes, and then centrifuged (300 g, 5 min). Following a 1-hour incubation period at 37ºC with 200 μL staining solution, the collected pellets are examined using a Gallios flow cytometer. Cells are taken and processed in accordance with the directions provided in the commercial annexin V-FITC/PI kit to measure apoptosis.
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| Animal Protocol |
female nude (nu/nu) Balb/C mice aged 6–8 weeks
25 mg/kg Oral gavage |
| References |
| Molecular Formula |
C15H15FN6O2S2
|
|---|---|
| Molecular Weight |
394.44
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| Exact Mass |
394.068
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| Elemental Analysis |
C, 45.68; H, 3.83; F, 4.82; N, 21.31; O, 8.11; S, 16.26
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| CAS # |
1421693-22-2
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| Related CAS # |
1421693-22-2
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| PubChem CID |
71561915
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.407
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
577
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1=C([H])C([H])=C([H])C(=C1[H])N([H])C1=NC([H])=C(C(C2=C(C([H])([H])[H])N=C(N([H])C([H])([H])[H])S2)=N1)F)(N([H])[H])(=O)=O
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| InChi Key |
GAIOPWBQKZMUNO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H15FN6O2S2/c1-8-13(25-15(18-2)20-8)12-11(16)7-19-14(22-12)21-9-4-3-5-10(6-9)26(17,23)24/h3-7H,1-2H3,(H,18,20)(H2,17,23,24)(H,19,21,22)
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| Chemical Name |
3-[[5-fluoro-4-[4-methyl-2-(methylamino)-1,3-thiazol-5-yl]pyrimidin-2-yl]amino]benzenesulfonamide
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| Synonyms |
CDKI73; CDKI-73; CDKI 73; asnuciclib [INN]; asnuciclib
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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: ~79 mg/mL (~200.3 mM)
Ethanol: ~1.5 mg/mL (~3.8 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.67 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 26.7 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5352 mL | 12.6762 mL | 25.3524 mL | |
| 5 mM | 0.5070 mL | 2.5352 mL | 5.0705 mL | |
| 10 mM | 0.2535 mL | 1.2676 mL | 2.5352 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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