Prexasertib Mesylate Hydrate

Modify Date: 2024-01-12 10:55:27

Prexasertib Mesylate Hydrate structure	Common Name	Prexasertib Mesylate Hydrate
	CAS Number	1234015-57-6	Molecular Weight	479.51
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₉H₂₅N₇O₆S	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Prexasertib Mesylate Hydrate

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a potent, selective, ATP competitive CHK1 and CHK2 inhibitor, with a Ki of 0.9 nM for CHK1 and IC50s of <1 nM, 8 nM for CHK1 and CHK2, respectively. Prexasertib Mesylate Hydrate inhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2 autophosphorylation (S516). Prexasertib Mesylate Hydrate shows potent anti-tumor activity, significantly abrogates the G2/M checkpoint in p53 deficient HeLa cells with an EC50 of 9 nM[1].

Name	Prexasertib Mesylate Hydrate
Synonym	More Synonyms

Description	Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a potent, selective, ATP competitive CHK1 and CHK2 inhibitor, with a Ki of 0.9 nM for CHK1 and IC50s of <1 nM, 8 nM for CHK1 and CHK2, respectively. Prexasertib Mesylate Hydrate inhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2 autophosphorylation (S516). Prexasertib Mesylate Hydrate shows potent anti-tumor activity, significantly abrogates the G2/M checkpoint in p53 deficient HeLa cells with an EC50 of 9 nM[1].
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> Checkpoint Kinase (Chk) Research Areas >> Cancer
Target	Chk1:0.9 nM (Ki) Chk1:<1 nM (IC50) Chk2:8 nM (IC50)
In Vitro	Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is an ATP competitive CHK1 inhibitor, with a Ki of 0.9 nM and an IC50 of <1 nM[1]. Prexasertib (LY2606368) shows high anti-tumor activity against U-2 OS, Calu-6 and HeLa cells (IC50, 3, 3, 37 nM, respectively), causes DNA damage during S-phase requiring CDC25A and CDK2 at 4 μM[1]. Prexasertib (0-20 nM) synergizes with olaparib (0-20 μM) to decrease cell viability in HGSOC cells[2].
Animal Admin	Prexasertib (1, 3.3 or 10 mg/kg s.c.) is well tolerated, and significantly inhibits tumor inhibition in mice bearing Calu-6 xenograft tumors[1].
References	[1]. King C, et al. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Mol Cancer Ther. 2015 Sep;14(9):2004-13. [2]. Brill E, et al. Prexasertib, a cell cycle checkpoint kinases 1 and 2 inhibitor, increases in vitro toxicity of PARP inhibition by preventing Rad51 foci formation in BRCA wild type high-grade serous ovarian cancer. Oncotarget. 2017 Oct 31;8(67):111026-111040.

Molecular Formula	C₁₉H₂₅N₇O₆S
Molecular Weight	479.51
Storage condition	2-8℃

Prexasertib (Mesylate Hydrate)

DC Chemicals Limited
China
Product Name: Prexasertib Mesylate Hydrate
Price: $Inquiry/250mg $Inquiry/100mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

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Prexasertib Mesylate Hydrate

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