1. Cell Cycle/DNA Damage
    Apoptosis
  2. CDK
    Apoptosis
  3. Samuraciclib hydrochloride

Samuraciclib hydrochloride (Synonyms: CT7001 hydrochloride; ICEC0942 hydrochloride)

Cat. No.: HY-103712A Purity: 99.98%
Handling Instructions

Samuraciclib hydrochloride (CT7001 hydrochloride; ICEC0942 hydrochloride) est un inhibiteur de CDK7 qui est puissant, sélectif, ATP-compétitif et oralement actif, avec un IC50 de 41 nM. Samuraciclib hydrochloride présente une sélectivité de 45, 15, 230 et 30 fois sur CDK1, CDK2 (IC50 de 578 nM), CDK5 et CDK9, respectivement. Samuraciclib hydrochloride inhibe la croissance des lignées cellulaires du cancer du sein avec des valeurs GI50 entre 0,2 et 0,3 µM. Samuraciclib hydrochloride a des effets anti-tumoraux.

Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 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.

For research use only. We do not sell to patients.

Samuraciclib hydrochloride Chemical Structure

Samuraciclib hydrochloride Chemical Structure

CAS No. : 1805789-54-1

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10 mM * 1 mL in DMSO USD 284 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
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Description

Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 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[1][2].

IC50 & Target

CDK7/cyclin H

41 nM (IC50)

cdk2/cyclin A

578 nM (IC50)

CDK1/cyc A

1.8 μM (IC50)

CDK4/Cyc D1

49 μM (IC50)

CDK5/p35NCK

9.4 μM (IC50)

CDK6/cycD1

34 μM (IC50)

CDK9/CycT1

1.2 μM (IC50)

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. ICEC0942 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 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].

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; female nu/nu-BALB/c athymic nude mice) 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) and ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts[1].

Animal Model: Female nu/nu-BALB/c athymic nude mice (7-week old) with MCF7 cells[1]
Dosage: 100 mg/kg
Administration: Oral gavage; daily; for 14 days
Result: At day 14, tumor growth was inhibited by 60%.
Clinical Trial
Molecular Weight

430.97

Formula

C₂₂H₃₁ClN₆O

CAS No.

1805789-54-1

SMILES

O[[email protected]]1CNCC[[email protected]@H]1CNC2=NC3=C(C(C)C)C=NN3C(NCC4=CC=CC=C4)=C2.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 62.5 mg/mL (145.02 mM)

H2O : 20 mg/mL (46.41 mM; ultrasonic and warming and heat to 80°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3203 mL 11.6017 mL 23.2035 mL
5 mM 0.4641 mL 2.3203 mL 4.6407 mL
10 mM 0.2320 mL 1.1602 mL 2.3203 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.98%

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Keywords:

SamuraciclibCT7001ICEC0942CT 7001CT-7001ICEC 0942ICEC-0942CDKApoptosisCyclin dependent kinaseCDK7phosphorylatesderegulationcycleAsp155PolIIanti-tumornon-covalentATP-competitivearrestInhibitorinhibitorinhibit

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Product Name:
Samuraciclib hydrochloride
Cat. No.:
HY-103712A
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