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) 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

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 284 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 490 In-stock
Estimated Time of Arrival: December 31
25 mg USD 980 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1600 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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[1][2]

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%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
Samuraciclib hydrochloride
Cat. No.:
HY-103712A
Quantity:
MCE Japan Authorized Agent: