Prexasertib Mesylate Hydrate salt form · mesylate · Parent LY2606368

Prexasertib Mesylate Hydrate is a selective, ATP-competitive second-generation checkpoint kinase 1 inhibitor.

For research use only. Not for human or veterinary use.

Target Checkpoint Kinase (Chk) Apoptosis

Research area Cancer

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Data Sheet SDS COA

Prexasertib Mesylate Hydrate structure

CAS No.: 1234015-57-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
10 mg	USD 320.00	BP-02309B-10mg	In stock	Get quote
25 mg	USD 640.00	BP-02309B-25mg	In stock	Get quote
50 mg	USD 1,020.00	BP-02309B-50mg	In stock	Get quote
100 mg	USD 1,640.00	BP-02309B-100mg	In stock	Get quote
250 mg	USD 3,280.00	BP-02309B-250mg	In stock	Get quote
500 mg	USD 5,250.00	BP-02309B-500mg	In stock	Get quote
1 g	Inquire	BP-02309B-1g	In stock	Inquire

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Description

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

Biological activity

In Vitro Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) 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. Prexasertib Mesylate Hydrate (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells. Prexasertib Mesylate Hydrate (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells. Prexasertib Mesylate Hydrate (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. Prexasertib Mesylate Hydrate (33 nM; for 12 hours) causes chromosomal fragmentation in HeLa cells. Prexasertib Mesylate Hydrate (100 nM; 0.5 to 9 hours) induces replication stress and depletes the pool of available RPA2 for binding to DNA. In Vivo Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate; 1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles) causes growth inhibition in tumor xenografts. Prexasertib Mesylate Hydrate (15 mg/kg; SC) causes CHK1 inhibition in the blood and the phosphorylation of both H2AX (S139) and RPA2 (S4/S8).

Identifiers

SMILES: N#CC1=NC=C(NC2=NNC(C3=C(OC)C=CC=C3OCCCN)=C2)N=C1.CS(=O)(O)=O.O
InChIKey: LCYWXOLNJNHLGN-UHFFFAOYSA-N

Specifications

MW (average): 479.5100
Formula: C₁₉H₂₅N₇O₆S
CAS No.: 1234015-57-6
Physical state: Solid
Color: White to yellow
Shipping: —
Storage: —

Documents

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].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.

Same target

Search Checkpoint Kinase (Chk)

Same research area

Search Cancer