Prexasertib dihydrochloride salt form · dihydrochloride · Parent LY2606368

Prexasertib dihydrochloride, LY2606368, 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 dihydrochloride structure

CAS No.: 1234015-54-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 500.00	BP-02309A-100mg	In stock	Get quote
250 mg	USD 750.00	BP-02309A-250mg	In stock	Get quote
1 g	USD 1,350.00	BP-02309A-1g	In stock	Get quote
5 g	Inquire	BP-02309A-5g	In stock	Inquire

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Description

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

Biological activity

Prexasertib (LY2606368) is a substrate ATP competitively selective inhibitor of CHK1 and CHK2 with IC50 values of <1 nM and 8 nM against CHK1 and CHK2, respectively. LY2606368 treatment led to TUNEL and pH2AXy positive double-stranded DNA breaks in cells in S phase. LY2606368 effectively cancelled the G2-M checkpoint activated by Doxorubicin in P53-deficient HeLa cells with EC50 of 9 nM. LY2606368 can play an antiproliferative role in a wide range of cells, with IC50s < 50 nM in most sensitive cell lines. Only a few cell lines were resistant to LY2606368, IC50s > 1000 nM. In vivo studies, LY2606368 can effectively inhibit tumor growth in tumor xenograft model and exert anti-tumor activity. In the SKOV3 ovarian cancer model, LY2606368 inhibited the growth of primary tumor and significantly reduced the rate of metastasis and ascites accumulation. In SW1990 model of pancreatic carcinoma in situ, LY2606368 inhibited the growth of 92% of the primary tumor and prevented its metastasis to lymph node tuberculosis, spleen and intestine.

Identifiers

SMILES: NCCCOC(C=CC=C1OC)=C1C2=CC(NC3=NC=C(C#N)N=C3)=NN2.[H]Cl.[H]Cl
InChIKey: KMEIPKXRCJTZBZ-UHFFFAOYSA-N

Specifications

MW (average): 438.3110
Formula: C₁₈H₂₁Cl₂N₇O₂
CAS No.: 1234015-54-3
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 4°C, sealed storage, away from moisture; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO H2O

In vitro: DMSO 8 mg/mL H2O < 0.1 mg/mL

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