This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
Samuraciclib
Catalog No. T61835 CAS
1805833-75-3
Samuraciclib (CT7001) is a potent, selective, and orally active inhibitor of CDK7, with an ATP-competitive nature. It effectively inhibits CDK7 with an IC 50 value of 41 nM. Furthermore, Samuraciclib demonstrates remarkable selectivity ratios, with 45-fold, 15-fold, 230-fold, and 30-fold selectivity over CDK1, CDK2 (IC 50 of 578 nM), CDK5, and CDK9, respectively. Notably, Samuraciclib has been found to inhibit the growth of breast cancer cell lines, exhibiting GI 50 values ranging between 0.2-0.3 μM. Additionally, Samuraciclib has been observed to possess anti-tumor effects [1] [2].
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage
& Solubility Information
Description
Samuraciclib (CT7001) is a potent, selective, and orally active inhibitor of CDK7, with an ATP-competitive nature. It effectively inhibits CDK7 with an IC 50 value of 41 nM. Furthermore, Samuraciclib demonstrates remarkable selectivity ratios, with 45-fold, 15-fold, 230-fold, and 30-fold selectivity over CDK1, CDK2 (IC 50 of 578 nM), CDK5, and CDK9, respectively. Notably, Samuraciclib has been found to inhibit the growth of breast cancer cell lines, exhibiting GI 50 values ranging between 0.2-0.3 μM. Additionally, Samuraciclib has been observed to possess anti-tumor effects [1] [2].
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, alongside significant decreases in PolII Ser2 and Ser5 phosphorylation levels in both PBMCs and tumors. Additionally, when combined with ICI 47699, Samuraciclib achieved complete inhibition of growth in estrogen receptor (ER)-positive tumor xenografts. This study utilized 7-week-old female nu/nu-BALB/c athymic nude mice implanted with MCF7 cells, demonstrating the compound's potent anticancer activity.
Molecular Weight
394.51
Formula
C22H30N6O
CAS No.
1805833-75-3
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dose Conversion
You can also refer to dose conversion for different animals.
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Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
Tween 80,mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL Corn oil,mix and clarify.
Note:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
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.