CCT245737 is an orally active and seletive Chk1 inhibitor, with an IC50 of 1.3 nM.
IC50&Target
Chk1
1.3 nM (IC50)
Chk2
2440 nM (IC50)
ERK8
130 nM (IC50)
PKD1
298 nM (IC50)
RSK2
361 nM (IC50)
RSK1
362 nM (IC50)
FLT3
582 nM (IC50)
MARK3
698 nM (IC50)
NUAK1
711 nM (IC50)
CLK2
1370 nM (IC50)
BRSK1
1660 nM (IC50)
AMPK
2970 nM (IC50)
PHK
3470 nM (IC50)
CDK2/CyclA
3850 nM (IC50)
CDK1/CyclB
9030 nM (IC50)
体外研究
CCT245737 (10 µM) shows >80% inhibition of a panel of 124 kinases, including ERK8, PKD1, RSK2 and RSK1 with IC50s of 130, 298, 361 and 362 nM. CCT245737 abrogates an VP-16-induced G2 checkpoint in HT29, SW620, MiaPaCa-2, and Calu6 cell lines, with IC50s ranging from 30 to 220 nM.
体内研究
CCT245737 (150 mg/kg p.o.) inhibits tumor growth in combination with LY 188011 (100 mg/kg iv) in HT29 colon cancer xenografts. CCT245737 (300 mg/kg, p.o.) also inhibits the LY 188011 (60 mg/kg iv) induced pSer296 CHK1 autophosphorylation at 24 h in SW620 human colon cancer xenografts. CCT245737 (150 mg/kg, p.o) alone significantly inhibits tumor growth in an Eμ-Myc mouse model of human B-cell lymphocytic leukemia.
分子式
C16H16N7OF3
分子量
379.34
CAS号
1489389-18-5
运输条件
Room temperature in continental US; may vary elsewhere.