All AbMole products are for research use only, cannot be used for human consumption.
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.
| 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 |
| Molecular Weight | 379.34 |
| Formula | C16H16F3N7O |
| CAS Number | 1489389-18-5 |
| Solubility (25°C) | DMSO ≥ 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Checkpoint Products |
|---|
| PV-1019
PV-1019 (NSC 744039) is a potent, selective Chk2 inhibitor with an IC50 value of 24 nM. PV-1019 inhibits IR-induced apoptosis. |
| CCT241533 dihydrochloride
CCT241533 dihydrochloride is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM. |
| CBP501 Affinity Peptide
CBP501 Affinity Peptide is a Chk kinase inhibitor that can abrogate G2 arrest induced by DNA-damaging agents. |
| Chktide
Chktide is a substrate for CHK1 and CHK2. |
| Zn-DPA-maytansinoid conjugate 1
Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
