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Prexasertib mesylate

Catalog No. T4310L2   CAS 1234015-55-4
Synonyms: LY-2606368, LY2606368, LY 2606368

Prexasertib is a potent and selective Chk1/Chk2 inhibitor. Prexasertib increases the effectiveness of conventional therapy in B-/T- cell progenitor acute lymphoblastic leukemia. LY2606368 causes replication catastrophe and antitumor effects through CHK1-dependent mechanisms. Treatment of cells with LY2606368 results in the rapid appearance of TUNEL and pH2AX-positive double-stranded DNA breaks in the S-phase cell population.

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Prexasertib mesylate Chemical Structure
Prexasertib mesylate, CAS 1234015-55-4
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,520.00
50 mg 6-8 weeks $ 1,980.00
100 mg 6-8 weeks $ 2,500.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Prexasertib is a potent and selective Chk1/Chk2 inhibitor. Prexasertib increases the effectiveness of conventional therapy in B-/T- cell progenitor acute lymphoblastic leukemia. LY2606368 causes replication catastrophe and antitumor effects through CHK1-dependent mechanisms. Treatment of cells with LY2606368 results in the rapid appearance of TUNEL and pH2AX-positive double-stranded DNA breaks in the S-phase cell population.
Targets&IC50 Chk1:<1 nM (IC50), Chk1:0.9 nM (Ki), Chk2:8 nM (IC50)
Synonyms LY-2606368, LY2606368, LY 2606368
Molecular Weight 461.49
Formula C19H23N7O5S
CAS No. 1234015-55-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Koppenhafer SL, Goss KL, Terry WW, Gordon DJ. mTORC1/2 and protein translation regulate levels of CHK1 and the sensitivity to CHK1 inhibitors in Ewing sarcoma cells. Mol Cancer Ther. 2018 Oct 3. pii: molcanther.0260.2018. doi: 10.1158/1535-7163.MCT-18-0260. [Epub ahead of print] PubMed PMID: 30282812. 2. Iwasa S, Yamamoto N, Shitara K, Tamura K, Matsubara N, Tajimi M, Lin AB, Asou H, Cai Z, Inoue K, Shibasaki Y, Saito K, Takai H, Doi T. Dose-finding study of the checkpoint kinase 1 inhibitor, prexasertib, in Japanese patients with advanced solid tumors. Cancer Sci. 2018 Oct;109(10):3216-3223. doi: 10.1111/cas.13750. PubMed PMID: 30040168. 3. Zhong B, Maharaj A, Davis A, Roussel MF, Stewart CF. Development and validation of a sensitive LC MS/MS method for the measurement of the checkpoint kinase 1 inhibitor prexasertib and its application in a cerebral microdialysis study. J Pharm Biomed Anal. 2018 Jul 15;156:97-103. doi: 10.1016/j.jpba.2018.04.018. Epub 2018 Apr 17. PubMed PMID: 29698863; PubMed Central PMCID: PMC5984718. 4. Hong DS, Moore K, Patel M, Grant SC, Burris HA 3rd, William WN Jr, Jones S, Meric-Bernstam F, Infante J, Golden L, Zhang W, Martinez R, Wijayawardana S, Beckmann R, Lin AB, Eng C, Bendell J. Evaluation of Prexasertib, a Checkpoint Kinase 1 Inhibitor, in a Phase Ib Study of Patients with Squamous Cell Carcinoma. Clin Cancer Res. 2018 Jul 15;24(14):3263-3272. doi: 10.1158/1078-0432.CCR-17-3347. Epub 2018 Apr 11. PubMed PMID: 29643063; PubMed Central PMCID: PMC6050086.

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Keywords

Prexasertib mesylate 1234015-55-4 LY-2606368 LY2606368 LY 2606368 Prexasertib Mesylate inhibitor inhibit

 

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