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CCT245737

Cat. No. M10129
CCT245737 Structure
Synonym:

SRA737; PNT-737

Size Price Availability Quantity
10mg USD 157  USD157 In stock
50mg USD 577  USD577 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

CCT245737 is a potent, selective and orally active checkpoint kinase 1 (CHK1) inhibitor, with IC50 values of 1.3 nM, 2440 nM and 30 nM for CHK1, CHK2 and G2 check point abrogation, respectively. CCT245737 (150 mg/kg, p.o) alone significantly inhibits tumor growth in an Eμ-Myc mouse model of human B-cell lymphocytic leukemia. CCT245737 (150 mg/kg, p.o.) inhibits tumor growth in combination with gemcitabine (100 mg/kg i.v.) in HT29 colon cancer xenografts. CCT245737 (300 mg/kg, p.o.) also inhibits the gemcitabine (60 mg/kg, i.v.) induced pSer296 CHK1 autophosphorylation at 24 h in SW620 human colon cancer xenografts.

Protocol
Cell Experiment
Cell lines HT29, SW620, MiaPaCa-2 and Calu6 cell line
Preparation method Cytotoxicity is determined as the drug concentration that gave 50% inhibition of tumor cell proliferation (GI50) using a 96h (i.e. 4-doublings) Sulforhodamine B (SRB) assay. Inhibition of intracellular CHK1 activity is measured using a cell based ELISA for the abrogation of an etoposide induced G2 checkpoint (mitosis induction assay, MIA).
Concentrations from 30 to 220nM
Incubation time 96 h
Animal Experiment
Animal models BALB/c mice
Formulation vehicle for oral administration of CCT245737 was DPTW (10% DMSO, 20% PEG400, 5% Tween 80 and 65% water)
Dosages 10mg/kg (i.v.); 150mg/kg (p.o.)
Administration i.v. or p.o. administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 379.34
Formula C16H16F3N7O
CAS Number 1489389-18-5
Purity >99%
Solubility DMSO ≥ 45 mg/mL
Storage at -20°C
References

[1] James D Osborne, et al. J Med Chem. Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737)

[2] Mike I Walton, et al. Oncotarget. The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphoma

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  Catalog
Abmole Inhibitor Catalog




Keywords: CCT245737, SRA737; PNT-737 supplier, Checkpoint, inhibitors

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