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

Samuraciclib trihydrochloride (Synonyms: CT7001 trihydrochloride; ICEC0942 trihydrochloride)

Cat. No.: HY-103712B Purity: 99.08%
Handling Instructions

Samuraciclib (CT7001) trihydrochloride is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib trihydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib trihydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib trihydrochloride has anti-tumor effects.

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

Samuraciclib trihydrochloride Chemical Structure

Samuraciclib trihydrochloride Chemical Structure

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 333 In-stock
Estimated Time of Arrival: December 31
Solid
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

Other Forms of Samuraciclib trihydrochloride:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Samuraciclib (CT7001) trihydrochloride is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib trihydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib trihydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib trihydrochloride has anti-tumor effects[1][2].

IC50 & Target[1][2]

CDK7

41 nM (IC50)

CDK2

578 nM (IC50)

CDK1

1.8 μM (IC50)

CDK4

49 μM (IC50)

CDK5

9.4 μM (IC50)

CDK6

31 μM (IC50)

CDK9

1.2 μM (IC50)

In Vitro

Samuraciclib trihydrochloride (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment promotes cell apoptosis[1].
Samuraciclib trihydrochloride (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment induces cell cycle arrest[1].
Samuraciclib trihydrochloride (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. Samuraciclib trihydrochloride also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma[1].
Samuraciclib trihydrochloride (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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, 0.01 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 trihydrochloride (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 trihydrochloride (ICEC0942) and ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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%.
Molecular Weight

503.90

Formula

C₂₂H₃₃Cl₃N₆O

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)

References

Purity: 99.08%

  • 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

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 *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Samuraciclib trihydrochloride
Cat. No.:
HY-103712B
Quantity:
MCE Japan Authorized Agent: