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Synonyms: (rel)-MC180295


| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $51 | In Stock | In Stock | |
| 5 mg | $133 | In Stock | In Stock | |
| 10 mg | $197 | In Stock | In Stock | |
| 25 mg | $335 | In Stock | In Stock | |
| 50 mg | $472 | In Stock | In Stock | |
| 100 mg | $672 | In Stock | In Stock | |
| 200 mg | $886 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $146 | In Stock | In Stock |
| Description | MC180295 ((rel)-MC180295) is a novel, potent, and highly selective CDK9 inhibitor with an IC50 of 5 nM, demonstrating over 22-fold selectivity compared to other CDKs. |
| Targets & IC50 | CDK2-CyclinE:367 nM, CDK6-CyclinD1:712 nM, CDK1-CyclinB:138 nM (cell free), CDK2-CyclinA:233 nM, CDK5-p25:186 nM (cell free), CDK4-CyclinD:112 nM (cell free), CDK9-CyclinT1:5 nM (cell free), CDK7-CyclinH-MAT1:555 nM, CDK3-CyclinE:399 nM, CDK5-p35:159 nM (cell free) |
| In vitro | MC180295 is a potent, selective CDK9-Cyclin T1 inhibitor with an IC50 of 5 nM, displaying at least 22-fold selectivity over other CDKs, including CDK1-Cyclin B (IC50, 138 nM), CDK2-Cyclin A (IC50, 233 nM), CDK2-Cyclin E (IC50, 367 nM), CDK3-Cyclin E (IC50, 399 nM), CDK4-Cyclin D (IC50, 112 nM), CDK5-P35 (IC50, 159 nM), and CDK5-P25 (IC50, 186 nM). MC180295 (0.1 μM) demonstrates broad anti-cancer activity in vitro. |
| In vivo | MC180295 (20 mg/kg, i.p., qod) demonstrates significant anti-tumor activity in mice with SW48 cells without inhibiting human T cell growth in vivo. |
| Synonyms | (rel)-MC180295 |
| Molecular Weight | 358.41 |
| Formula | C17H18N4O3S |
| Cas No. | 2237942-08-2 |
| Smiles | Nc1nc(N[C@H]2C[C@@H]3CC[C@H]2C3)sc1C(=O)c1ccccc1[N+]([O-])=O |
| Relative Density. | 1.462 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 150 mg/mL (418.52 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: < 10 mg/mL (27.9 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (27.9 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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