Samuraciclib hydrochloride hydrate (Synonyms: CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate) |
Katalog-Nr.GC63736
One-Click Copy Product Info
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Samuraciclib (CT7001) Hydrochloridhydrat ist ein potenter, selektiver, ATP-kompetitiver und oral aktiver CDK7-Inhibitor mit einem IC50 von 41 nM. Samuraciclib-Hydrochloridhydrat zeigt eine 45-, 15-, 230- und 30-fache SelektivitÄt gegenÜber CDK1, CDK2 (IC50 von 578 nM), CDK5 bzw. CDK9. Samuraciclib-Hydrochloridhydrat hemmt das Wachstum von Brustkrebszelllinien mit GI50-Werten zwischen 0,2-0,3 μM. Samuraciclib-Hydrochloridhydrat hat Antitumorwirkungen.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride hydrate has anti-tumor effects[1][2].
Samuraciclib hydrochloride hydrate (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment promotes cell apoptosis[1].Samuraciclib hydrochloride hydrate (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment induces cell cycle arrest[1].Samuraciclib hydrochloride hydrate (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 trihydrochloride also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma[1].Samuraciclib (ICEC0942) hydrochloride hydrate inhibits the growth of MCF7, T47D, MDA-MB-231, HS578T, MDA-MB-468, MCF10A and HMEC cells with GI50 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].
Samuraciclib (ICEC0942; 100 mg/kg; oral gavage; daily; for 14 days; female nu/nu-BALB/c athymic nude mice) hydrochloride hydrate treatment inhibits tumor growth by 60% at day 14, and is accompanied by highly significant reductions in PolII Ser2 and Ser5 phosphorylation in PBMCs and in tumors[1].The combination of Samuraciclib (ICEC0942) hydrochloride hydrate and ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts[1].
[1]. Patel H, et al. ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment. Mol Cancer Ther. 2018 Jun;17(6):1156-1166.
[2]. Hazel P, et al. Inhibitor Selectivity for Cyclin-Dependent Kinase 7: A Structural, Thermodynamic, and Modelling Study. ChemMedChem. 2017 Mar 7;12(5):372-380.
| Cas No. | SDF | ||
| Überlieferungen | CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate | ||
| Formula | C22H30N6O.(2.5HCl).(2H2O) | M.Wt | 521.7 |
| Löslichkeit | DMSO : 100 mg/mL (191.68 mM; Need ultrasonic) | Storage | 4°C, stored under nitrogen, away from moisture |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9168 mL | 9.5841 mL | 19.1681 mL |
| 5 mM | 383.4 μL | 1.9168 mL | 3.8336 mL |
| 10 mM | 191.7 μL | 958.4 μL | 1.9168 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)