ChemicalBook CAS DataBase List 1234015-58-7

1234015-58-7

Name	Prexasertib dimesylate
CAS	1234015-58-7
Molecular Formula	C19H23N7O5S
MDL Number	MFCD32693943
Molecular Weight	461.5
MOL File	1234015-58-7.mol

Chemical Properties

form	Solid
color	Light yellow to yellow

Hazard Information

Uses

Prexasertib dimesylate (LY2606368 dimesylate) 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 dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity[1][2].

in vivo

Prexasertib dimesylate (LY2606368 dimesylate; 1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles) causes growth inhibition in tumor xenografts^[1].
Prexasertib dimesylate (15 mg/kg; SC) causes CHK1 inhibition in the blood and the phosphorylation of both H2AX (S139) and RPA2 (S4/S8)^[1].

Animal Model:	Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells^[1]
Dosage:	1, 3.3, or 10 mg/kg
Administration:	SC; twice daily for 3 days, rest 4 days; for three cycles
Result:	Caused statistically significant tumor growth inhibition (up to 72.3%).

Animal Model:	Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells^[1]
Dosage:	15 mg/kg (Pharmacokinetic Analysis)
Administration:	SC (200 μL)
Result:	CHK1 was 7 ng/mL at 12 hours and 3 ng/mL by 24 hours in plasma exposures. Phosphorylation of both H2AX (S139) and RPA2 (S4/S8) was detectable at 4 hours, showing the rapid occurrence of DNA damage.

IC 50

Chk1: 0.9 nM (Ki); Chk1: <1 nM (IC₅₀); Chk2: 8 nM (IC₅₀)

References

[1] King C, et al. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Mol Cancer Ther. 2015 Sep;14(9):2004-1 DOI:10.1158/1535-7163.MCT-14-1037
[2] Yin Y, et al. Chk1 inhibition potentiates the therapeutic efficacy of PARP inhibitor BMN673 in gastric cancer. Am J Cancer Res. 2017 Mar 1;7(3):473-483. PMID:28401005

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