Prexasertib dihydrochloride_product_DataBase

Bioactivity	Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity[1][2].
Invitro	Prexasertib dihydrochloride (LY2606368 dihydrochloride) inhibits MELK (IC50=38 nM), SIK (IC50=42 nM), BRSK2 (IC50=48 nM), ARK5 (IC50=64 nM). LY2606368 requires CDC25A and CDK2 to cause DNA damage[1]. Prexasertib dihydrochloride (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells[1]. Prexasertib dihydrochloride (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells[1]. Prexasertib dihydrochloride (4 nM; 24 hours) results in a large shift in cell-cycle populations from G1 and G2-M to S-phase with an accompanied induction of H2AX phosphorylation in U-2 OS cells[1]. Prexasertib dihydrochloride (33 nM; for 12 hours) causes chromosomal fragmentation in HeLa cells. Prexasertib (100 nM; 0.5 to 9 hours) induces replication stress and depletes the pool of available RPA2 for binding to DNA[1]. Cell Cycle Analysis[1] Cell Line:
Name	Prexasertib dihydrochloride
CAS	1234015-54-3
Formula	C18H21Cl2N7O2
Molar Mass	438.31
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

PeptideDB

Prexasertib dihydrochloride

CAS: 1234015-54-3 F: C18H21Cl2N7O2 W: 438.31