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Samuraciclib
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Catalog No. T61835Cas No. 1805833-75-3
Samuraciclib (CT7001) is a potent, selective, and orally active CDK7 inhibitor with an ATP-competitive nature, effectively inhibiting CDK7 with an IC50 of 41 nM. It demonstrates 45-fold, 15-fold (IC50 of 578 nM), 230-fold, and 30-fold selectivity over CDK1, CDK2, CDK5, and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values of 0.2-0.3 μM and possesses anti-tumor effects [1] [2].
Samuraciclib
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Catalog No. T61835Cas No. 1805833-75-3
Samuraciclib (CT7001) is a potent, selective, and orally active CDK7 inhibitor with an ATP-competitive nature, effectively inhibiting CDK7 with an IC50 of 41 nM. It demonstrates 45-fold, 15-fold (IC50 of 578 nM), 230-fold, and 30-fold selectivity over CDK1, CDK2, CDK5, and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values of 0.2-0.3 μM and possesses anti-tumor effects [1] [2].
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | 10-14 weeks | 10-14 weeks | |
| 50 mg | $1,980 | 10-14 weeks | 10-14 weeks | |
| 100 mg | $2,500 | 10-14 weeks | 10-14 weeks |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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| Description | Samuraciclib (CT7001) is a potent, selective, and orally active CDK7 inhibitor with an ATP-competitive nature, effectively inhibiting CDK7 with an IC50 of 41 nM. It demonstrates 45-fold, 15-fold (IC50 of 578 nM), 230-fold, and 30-fold selectivity over CDK1, CDK2, CDK5, and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values of 0.2-0.3 μM and possesses anti-tumor effects [1] [2]. |
| Targets&IC50 | CDK4:49 μM, CDK5:9.4 μM, CDK1:1.8 μM, CDK9:1.2 μM, CDK2-CyclinE1:578 nM, CDK7-CyclinH-MAT1:41 nM, CDK6:34 μM |
| In vitro | Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment promotes cell apoptosis [1]. Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment induces cell cycle arrest [1]. Samuraciclib (ICEC0942; 0-10 μM; 0-24 hours; HCT116 cells) treatment inhibits the phosphorylation of PolII CTD in a dose and time dependent manner in HCT116 colon cancer cells. Samuraciclib also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma [1]. Samuraciclib (ICEC0942) inhibits the growth of MCF7, T47D, MDA-MB-231, HS578T, MDA-MB-468, MCF10A and HMEC cells with GI 50 values of 0.18 μM, 0.32 μM, 0. 33 μM, 0.21 μM, 0.22 μM, 0.67 μM and 1.25 μM, respectively [1]. Apoptosis Analysis [1] Cell Line: HCT116 cells Concentration: 0 μM, 0.1 μM, 1 μM and 10 μM Incubation Time: 24 hours Result: Induced caspase 3/7 and demonstrated PARP cleavage. Cell Cycle Analysis [1] Cell Line: HCT116 cells Concentration: 0 μM, 0.01 μM, 0.1 μM, 1 μM and 10 μM Incubation Time: 24 hours Result: Showed accumulation of cells in G2/M. Western Blot Analysis [1] Cell Line: HCT116 cells Concentration: 0 μM, 0.1 μM, 1 μM and 10 μM Incubation Time: 0 hour, 4 hours, 8 hours, 16 hours or 24 hours Result: PolII CTD phosphorylation was inhibited in a dose and time dependent manner in HCT116 colon cancer cells. |
| In vivo | Samuraciclib (ICEC0942; 100 mg/kg; oral gavage; daily; for 14 days) administered to female nu/nu-BALB/c athymic nude mice resulted in a 60% inhibition of tumor growth by day 14, with significant decreases in PolII Ser2 and Ser5 phosphorylation levels in both PBMCs and tumors. Combined with ICI 47699, Samuraciclib achieved complete inhibition of growth in estrogen receptor (ER)-positive tumor xenografts. This study, utilizing 7-week-old female nu/nu-BALB/c athymic nude mice implanted with MCF7 cells, demonstrates the compound's potent anticancer activity. |
| Molecular Weight | 394.51 |
| Formula | C22H30N6O |
| Cas No. | 1805833-75-3 |
| Smiles | N(CC1=CC=CC=C1)C=2N3C(=C(C(C)C)C=N3)N=C(NC[C@@H]4[C@@H](O)CNCC4)C2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
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.
Preparation of the In Vivo Formulation:
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.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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