| Identification | Back 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 |
| Hazard Information | Back 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%).
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| [IC 50]
Chk1: 0.9 nM (Ki); Chk1: <1 nM (IC50); Chk2: 8 nM (IC50) |
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| Company Name: |
BOC Sciences
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| Tel: |
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| Website: |
https://www.bocsci.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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