ChemicalBook > CAS DataBase List > 5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile hydrochloride

5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile hydrochloride

Product Name: 5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile hydrochloride
CAS No.: 1234015-54-3
Chemical Name: 5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile hydrochloride
Synonyms: Prexasertib HCl;LY2606368 dihydrochloride;LY2606368 2HCL;LY 2606368;LY-2606368;LY-2606368 (Prexasertib);LY-2606368 dihydrochloride;Prexasertib dihydrochloride;Prexasertib HCl (LY2606368);Prexasertib (LY2606368) 2HCl;Prexasertib 2HCl (LY-2606368)
CBNumber: CB02669661
Molecular Formula: C18H21Cl2N7O2
Formula Weight: 438.31104
MOL File: 1234015-54-3.mol

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5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile hydrochloride Property

storage temp.: Inert atmosphere,Store in freezer, under -20°C
solubility: DMSO:12.5(Max Conc. mg/mL);28.52(Max Conc. mM)
form: Solid
color: Light yellow to yellow

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-3507
Product name: Prexasertib(dihydrochloride)
Purity: 99.41%
Packaging: 5mg
Price: $110
Updated: 2021/12/16

ChemScene

Product number: CS-3507
Product name: Prexasertib(dihydrochloride)
Purity: 99.41%
Packaging: 10mg
Price: $180
Updated: 2021/12/16

ApexBio Technology

Product number: B8313
Product name: 5-((5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile hydrochloride
Packaging: 5mg
Price: $220
Updated: 2021/12/16

AK Scientific

Product number: 4999DG
Product name: Prexasertibdihydrochloride
Packaging: 50mg
Price: $316
Updated: 2021/12/16

ChemScene

Product number: CS-3507
Product name: Prexasertib(dihydrochloride)
Purity: 99.41%
Packaging: 25mg
Price: $350
Updated: 2021/12/16

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5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile hydrochloride Chemical Properties,Usage,Production

Description

Prexasertib HCl is a member of the serine/threonine protein kinase family and is the core protein of cell cycle checkpoints in DNA damage response (DDR).

Uses

Prexasertib dihydrochloride (LY2606368 dihydrochloride) 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[1][2].

Biological Activity

Prexasertib HCl is an ATP-competitive inhibitor of CHK1 with a Ki value of 0.9 nM. In cell-free experiments, the IC50 values of it for CHK2 and RSK were 8 nM and 9 nM, respectively.

in vivo

Prexasertib dihydrochloride (LY2606368 dihydrochloride; 1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles) causes growth inhibition in tumor xenografts^[1].
? Prexasertib dihydrochloride (15 mg/kg; SC) causes CHK1 inhibition in the blood and the phosphorylation of both H2AX (S139) and RPA2 (S4/S8)^[1].

Animal Model:	Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells^[1]
Dosage:	1, 3.3, or 10 mg/kg
Administration:	SC; twice daily for 3 days, rest 4 days; for three cycles
Result:	Caused statistically significant tumor growth inhibition (up to 72.3%).

Animal Model:	Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells^[1]
Dosage:	15 mg/kg (Pharmacokinetic Analysis)
Administration:	SC (200 μL)
Result:	CHK1 was 7 ng/mL at 12 hours and 3 ng/mL by 24 hours in plasma exposures. Phosphorylation of both H2AX (S139) and RPA2 (S4/S8) was detectable at 4 hours, showing the rapid occurrence of DNA damage.

target

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Target	Value
Chk1 (Cell-free assay)	0.9 nM(Ki)
Chk2 (Cell-free assay)	8 nM
RSK (Cell-free assay)	9 nM

IC 50

Chk1: 0.9 nM (Ki); Chk1: <1 nM (IC₅₀); Chk2: 8 nM (IC₅₀)

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 DOI:10.1158/1535-7163.MCT-14-1037
[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. PMID:28401005

5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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1234015-54-3, 5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile hydrochlorideRelated Search:

L-LEUCYL-L-TYROSINE THZ1 (Hydrochloride) RMC6291

5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile hydrochloride

5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile dihydrochloride

LY2606368 dihydrochloride

LY-2606368 dihydrochloride

Prexasertib (LY2606368) 2HCl

Prexasertib HCl (LY2606368)

Prexasertib dihydrochloride

LY-2606368 (Prexasertib)

LY 2606368;LY-2606368

LY 2606368;LY-2606368;PREXASERTIB DIHYDROCHLORIDE

Prexasertib HCl

LY2606368 2HCL

Prexasertib 2HCl (LY-2606368)

Apoptosis,CDK2,Prexasertib,ARK5,replication,RSK1,inhibit,MELK,DNA,HeLa,LY 2606368,Inhibitor,Prexasertib dihydrochloride,HT-29,double-stranded,BRSK2,ATP-competitive,CDC25A,S296,S516,autophosphorylation,H2AX,LY-2606368,SIK,Checkpoint Kinase (Chk)

Prexasertib dihydrochloride, 10 mM in DMSO

Prexasertib 2HCl (LY2606368 dihydrochloride)

Prexasertib HCl (LY2606368) ，S7178

Prexasertib dihydrochloride (LY-2606368 dihydrochloride

Prexasertib hydrochloride (LY2606368)

1234015-54-3