1333377-65-3 Usage
Description
CHR-6494 is a haspin protein kinase inhibitor (IC50 = 2 nM) selective over 27 other protein kinases, including Aurora B kinase (IC50 > 1 μM). Haspin is a kinase necessary for mitosis that selectively phosphorylates histone 3 at the threonine 3 residue (H3T3ph). CHR-6494 decreases phosphorylation of H3T3 and arrests the cell cycle in the G2/M phase, which leads to apoptosis. It showed promising results in a xenograft tumor model.
Uses
CHR6494 is a small-molecule inhibitor of histone kinase haspin, with a wide spectrum of anticancer effects.
General Description
A cell-permeable indazolylimidazopyridazinamine compound that acts as a potent and reversible inhibitor of histone kinase haspin activity (IC50 = 2 nM) with moderate selectivity over TrkA, GSK-3β, PIM1, Cdk1/B and Cdk2/A (% inhibition at 100 nM = 58, 48, 36, 34 and 33, respectively) among a panel of 27-kinases. Shown to block pH3-Thr3, with no effect on pH3-Ser10 and pH3-Ser28, cause mitotic catastrophe, upregulate BUB1 and cyclin B1 levels, and potently induce apoptosis (IC50 = 473, 500 and 752 nM in HeLa, HCT-116 and MDA-MB-231 cells, respectively). Further, efficiently blocks bFGF-induced sprouting vessel by 70% at 1 μM (chicken embryo aortic arch ring assay) and suppresses tumor growth in HCT-116 xenografted mouse model (50 mg/kg, i.p.).
Check Digit Verification of cas no
The CAS Registry Mumber 1333377-65-3 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,3,3,3,7 and 7 respectively; the second part has 2 digits, 6 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 1333377-65:
(9*1)+(8*3)+(7*3)+(6*3)+(5*3)+(4*7)+(3*7)+(2*6)+(1*5)=153
153 % 10 = 3
So 1333377-65-3 is a valid CAS Registry Number.
