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
ApexBio Technology
Product number
B8313
Product name
5-((5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile hydrochloride
Packaging
25mg
Price
$660
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

< tr>
TargetValue
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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5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile hydrochloride Suppliers

China 72 United States 7 Global 79
Haoyuan Chemexpress Co., Ltd.
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021-58950125
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(86) 21-58955996
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China
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MedChemexpress LLC
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021-58955995
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609-228-5909
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sales@medchemexpress.cn
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United States
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CEG Chemical Science&Technology Co., Ltd.
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Mobile:13665161512
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+86-510-68873513
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China
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ShangHai Caerulum Pharma Discovery Co., Ltd.
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18149758185
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sales-cpd@caerulumpharma.com
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China
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Shanghai XR Chemical Technology Co., Ltd.
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021-31007982 18019432809
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LETOPHARM LIMITED
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Shanghai YuanQi Biotechnology Co., Ltd.
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+86-2332782371 +86-18120098618
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Shanghaizehan biopharma technology co., Ltd.
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020-61288194 61288195
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020-61288700
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505721671@qq.com
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Shanghai YuanYe Biotechnology Co., Ltd.
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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

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