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1234015-55-4

1234015-55-4 Structure

1234015-55-4 Structure
IdentificationBack Directory
[Name]

Prexasertib mesylate
[CAS]

1234015-55-4
[Synonyms]

LY2606368 mesylate
Prexasertib mesylate
Prexasertib mesylate (LY-2606368 mesylate)
5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2-carbonitrile mesylate
[Molecular Formula]

C19H23N7O5S
[MOL File]

1234015-55-4.mol
[Molecular Weight]

461.5
Chemical PropertiesBack Directory
[solubility ]

DMSO:24.0(Max Conc. mg/mL);52.0(Max Conc. mM)
Hazard InformationBack Directory
[Uses]

Prexasertib Mesylate is a novel CHK1 inhibitor under investigation as a chemopotentiating agent. It causes double-stranded DNA breakage while simultaneously removing the protection of the DNA damage checkpoints. Prexasertib Mesylate is representative of a novel class of drugs for the treatment of cancer and tumor growth inhibition.
[in vivo]

Prexasertib mesylate (1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles) causes growth inhibition in tumor xenografts[1].
Prexasertib mesylate (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%).
[IC 50]

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