[CAS NO. 905973-89-9]  CGK733

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PRODUCTS SPECIFICATIONS [905973-89-9]

Catalog
HY-15520
Brand
MCE
CAS
905973-89-9

DESCRIPTION [905973-89-9]

Overview

MDLMFCD09038682
Molecular Weight555.84
Molecular FormulaC23H18Cl3FN4O3S
SMILESFC1=CC=C(NC(NC(C(Cl)(Cl)Cl)NC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)=S)C=C1[N+]([O-])=O

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


Summary

CGK733 is a potent ATM/ATR inhibitor, used for the research of cancer .


IC50 & Target

ATM

ATR


In Vitro

CGK733 (4.2 ng/μL-12.5 ng/μL) enhances taxol-induced cytotoxicity in HBV-positive HCC cells. CGK733 (4.2 ng/μL) accelerates the formation of multinucleated cells and promotes the exit of mitosis in taxol-treated HBV-positive HCC cells [1] . CGK733 (10 μM) causes the loss of cyclin D1 through the ubiquitin-dependent proteasomal degradation pathway in MCF-7 and T47D breast cancer cell lines. CGK733 (0.6-40 μM) shows inhibitory activities against proliferation of LnCap prostate cancer cells, HCT116 colon cancer cells, MCF-7 and T47D estrogen receptor positive breast cancer cells, and MDA-MB436 ER negative breast cancer cells. Moreover, CGK733 inhibits proliferation of non-transformed mouse BALB/c 3T3 embryonic fibroblast cells. In addition, CGK733 (10 μM) inhibits MCF-7 proliferation, and the effect can not be suppressed by pan-caspase inhibition [2] . CGK733 (10 μM) results in 1.6-fold increase in ATM reporter activity in HEK-293 cells [3] .

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


In Vivo

CGK733 (25 mg/kg, i.p.) increases the ATM reporter activity (reports inactivation of ATM kinase activity) compared to control mice, with 2.4-fold, 3.1-fold, and 1.3-fold changes at 1, 4, and 8 hours, respectively [3] .

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


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 179.91 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7991 mL 8.9954 mL 17.9908 mL
5 mM 0.3598 mL 1.7991 mL 3.5982 mL
10 mM 0.1799 mL 0.8995 mL 1.7991 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

* All of the co-solvents are available by MCE.