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Samuraciclib hydrochloride
🥰Excellent
Catalog No. T10898Cas No. 1805789-54-1
Alias ICEC0942 hydrochloride, CT7001 hydrochloride
Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.
Samuraciclib hydrochloride
🥰Excellent
Purity: 99.8%
Catalog No. T10898Alias ICEC0942 hydrochloride, CT7001 hydrochlorideCas No. 1805789-54-1
Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $116 | In Stock | |
| 5 mg | $247 | In Stock | |
| 10 mg | $396 | In Stock | |
| 25 mg | $662 | In Stock | |
| 50 mg | $942 | In Stock | |
| 100 mg | $1,280 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $273 | In Stock |
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Purity:99.8%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects. |
| Targets&IC50 | CDK6-CyclinD1:34 μM, CDK4-CyclinD1:49 μM, CDK9-CyclinT1:1.2 μM, CDK7-CyclinH:41 nM, CDK2-CyclinA:578 nM, CDK5-p35 NCK:9.4 μM, CDK1-CyclinA:1.8 μM |
| In vitro | Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment can promote apoptosis. Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment can induce cell cycle arrest. Samuraciclib (ICEC0942; 0-10 μM; 0-24 hours; HCT116 cells) treatment inhibited the phosphorylation of PolII CTD in HCT116 colon cancer cells in a dose- and time-dependent manner. ICEC0942 also inhibits the phosphorylation of CDK1, CDK2 and retinoblastoma. Samuraciclib (ICEC0942) 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 It is 0.67 μM and 1.25 μM. |
| In vivo | 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. |
| Alias | ICEC0942 hydrochloride, CT7001 hydrochloride |
| Molecular Weight | 430.97 |
| Formula | C22H31ClN6O |
| Cas No. | 1805789-54-1 |
| Smiles | Cl.CC(C)c1cnn2c(NCc3ccccc3)cc(NC[C@H]3CCNC[C@@H]3O)nc12 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: 55 mg/mL (127.62 mM), Sonication is recommended. DMSO: 25 mg/mL (58.01 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/H2O
H2O
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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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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Keywords
Samuraciclib HydrochlorideSamuraciclib hydrochlorideSamuraciclibPolIIphosphorylatesnon-covalentInhibitorinhibitICEC-0942 HydrochlorideICEC0942 HydrochlorideICEC-0942ICEC0942ICEC 0942 HydrochlorideICEC 0942deregulationCyclin dependent kinasecycleCT-7001 HydrochlorideCT7001 HydrochlorideCT-7001CT7001CT 7001 HydrochlorideCT 7001CDK7CDKATP-competitiveAsp155arrestApoptosisanti-tumor
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