Structure
Samuraciclib hydrochloride, Inhibitor
Samuraciclib hydrochloride
Purity
98.00%
Synonyms
Samuraciclib hydrochloride; CT7001 hydrochloride; ICEC0942 hydrochloride; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 62.5mg/mL (145.02mM)
H2O: 20mg/mL (46.41mM) ultrasonic and warming and heat to 80 degree C
(<1mg/ml refers to the product slightly soluble or insoluble)
H2O: 20mg/mL (46.41mM) ultrasonic and warming and heat to 80 degree C
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C22H31ClN6O
SMILES
O[C@H]1CNCC[C@@H]1CNC2=NC3=C(C(C)C)C=NN3C(NCC4=CC=CC=C4)=C2.[H]Cl
CAS Number
1805789-54-1
Target & IC50
CDK7/cyclin H: ic50 41nM
cdk2/cyclin A: ic50 578nM
CDK1/cyc A: ic50 1.8uM
CDK4/Cyc D1: ic50 49uM
CDK5/p35NCK: ic50 9.4uM
CDK6/cycD1: ic50 34uM
CDK9/CycT1: ic50 1.2uM
cdk2/cyclin A: ic50 578nM
CDK1/cyc A: ic50 1.8uM
CDK4/Cyc D1: ic50 49uM
CDK5/p35NCK: ic50 9.4uM
CDK6/cycD1: ic50 34uM
CDK9/CycT1: ic50 1.2uM
In Vitro
Samuraciclib (ICEC0942; 100 mg/kg; oral tube; daily; 14 consecutive days; female nu/nu-BALB/c athymic nude mice) treatment,inhibited tumor growth by 60% on day 14 with a significant reduction in PolII Ser2 and Ser5 phosphorylation in PBMC and tumors. The combination of Samuraciclib (ICEC0942) and ICI 47699 treatment, showed complete stagnation of estrogen receptor (ER) positive tumor xenografts.
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Structure
Structure
Related Product Information for Samuraciclib hydrochloride, inhibitor
Samuraciclib hydrochloride (CT7001 hydrochloride; ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3uM. Samuraciclib hydrochloride has anti-tumor effects.
Product Categories/Family for Samuraciclib hydrochloride, inhibitor
References
Patel H, et al. ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer treatment, Mol Cancer Ther. 2018 Jun;17(6):1156-1166.
Patel H, et al. ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer treatment, Mol Cancer Ther. 2018 Jun;17(6):1156-1166.
Hazel P, et al. Inhibitor Selectivity for Cyclin-Dependent Kinase7: AStructural, Thermodynamic, and Modelling Study. ChemMedChem. 2017 Mar 7;12(5):372-380.
Hazel P, et al. Inhibitor Selectivity for Cyclin-Dependent Kinase7: AStructural, Thermodynamic, and Modelling Study. ChemMedChem. 2017 Mar 7;12(5):372-380.
Patel H, et al. ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer treatment, Mol Cancer Ther. 2018 Jun;17(6):1156-1166.
Hazel P, et al. Inhibitor Selectivity for Cyclin-Dependent Kinase7: AStructural, Thermodynamic, and Modelling Study. ChemMedChem. 2017 Mar 7;12(5):372-380.
Hazel P, et al. Inhibitor Selectivity for Cyclin-Dependent Kinase7: AStructural, Thermodynamic, and Modelling Study. ChemMedChem. 2017 Mar 7;12(5):372-380.
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Product Notes
The Samuraciclib hydrochloride (Catalog #AAA5752956) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "Samuraciclib hydrochloride, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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