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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 |
|---|
| AZD7762
AZD7762 is a potent ATP-competitive checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for CHK1 and CHK2 respectively. |
| BIBR1532
BIBR1532 is a potent and selective telomerase inhibitor with IC50 of 100 nM. BIBR 1532 inhibits the proliferation of JVM13 leukemia cells with an IC50 of 52 μM, and similar effect also occurs in other leukemia cell lines such as Nalm-1, HL-60, and Jurkat. BIBR1532 is also an inhibitor of TERT, the rate-limiting enzyme in the regulation of telomerase activity. |
| PF-477736
PF-477736 is a selective checkpoint kinase 1 (Chk1) inhibitor with Ki values of 0.49 nM and 47 nM for CHK1 and CHK2 respectively. |
| SCH 900776
SCH 900776 (MK-8776) is a highly potent and functionally selective CHK1 inhibitor with IC50 of 3 nM. |
| Rabusertib (LY2603618)
Rabusertib (LY2603618) is an effective and selective Chk1 inhibitor with an IC50 of 7 nM. |
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