LY2606368 free base · Synonyms: Prexasertib

Prexasertib 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

Purity >98% Stock Inquire

Data Sheet SDS COA

LY2606368 structure

CAS No.: 1234015-52-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 480.00	BP-02309-100mg	In stock	Get quote
250 mg	USD 960.00	BP-02309-250mg	In stock	Get quote
500 mg	USD 1,520.00	BP-02309-500mg	In stock	Get quote
1 g	USD 2,450.00	BP-02309-1g	In stock	Get quote
2 g	USD 3,930.00	BP-02309-2g	In stock	Get quote
3 g	USD 4,710.00	BP-02309-3g	In stock	Get quote
5 g	USD 6,290.00	BP-02309-5g	In stock	Get quote

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Related forms

BP-02309A — Prexasertib dihydrochloride

Description

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

Biological activity

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

Identifiers

SMILES: COC1=C(C2=CC(NC3=CN=C(C=N3)C#N)=NN2)C(OCCCN)=CC=C1
InChIKey: DOTGPNHGTYJDEP-UHFFFAOYSA-N

Specifications

MW (average): 365.3892
Formula: C₁₈H₁₉N₇O₂
CAS No.: 1234015-52-1
Physical state: Solid
Color: Light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

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):2004-1

[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