Samuraciclib hydrochloride

SKU: orb1309808

Description

Samuraciclib hydrochloride is a potent, orally bioavailable and selective CDK7 inhibitor (IC50=41 nM). It demonstrates anti-proliferative activity in breast cancer cell lines (GI50 0.2-0.3 µM) and has shown antitumor efficacy in preclinical in vivo studies.

Research Area

Cell Biology

Key Properties

• CAS Number: 1805789-54-1
• MW: 430.97
• Purity: 99.80% (May vary between batches)
• Formula: C₂₂H₃₁ClN₆O
• SMILES: Cl.CC(C)c1cnn2c(NCc3ccccc3)cc(NC[C@H]3CCNC[C@@H]3O)nc12
• Target: CDK,Apoptosis
• Solubility: H2O:55 mg/mL (127.62 mM);DMSO:150 mg/mL (348.05 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.64 mM)

Bioactivity

• Target IC50:
  CDK6-CyclinD1:34 μM|CDK9-CyclinT1:1.2 μM|CDK4-CyclinD1:49 μM|CDK5-p35 NCK:9.4 μM|CDK2-CyclinA:578 nM|CDK7-CyclinH:41 nM|CDK1-CyclinA:1.8 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.
• 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.

Storage & Handling

• 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/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CT7001, CT-7001, CT7001 hydrochloride, CT7001 Hydrochloride, CT-7001 Hydrochloride, CT 7001, CT 7001 Hydrochloride, cycle, Cyclin dependent kinase, deregulation, CDK4/Cyc D1, cdk2/cyclin A, CDK2/cyclinA, CDK5/p35NCK, CDK6/cycD1, CDK7, CDK7/cyclinH, CDK7/cyclin H, CDK9/CycT1, CDK, CDK1/cyc A, Apoptosis, anti-tumor, ATP-competitive, Asp155, arrest, non-covalent, inhibit, ICEC 0942, ICEC 0942 Hydrochloride, ICEC0942, ICEC-0942, ICEC0942 hydrochloride, ICEC0942 Hydrochloride, ICEC-0942 Hydrochloride, Inhibitor, Samuraciclib, Samuraciclib hydrochloride, Samuraciclib Hydrochloride, PolII, phosphorylates

Compound Identifiers

PubChem CID

91844732