ChemicalBook > CAS DataBase List > LY 2606368

LY 2606368

Product Name
LY 2606368
CAS No.
1234015-52-1
Chemical Name
LY 2606368
Synonyms
CS-1453;LY 2606368;Prexasertib;Prexasertib free base;Prexasertib (LY2606368);LY2606368 HCl(free base);LY 2606368;LY-2606368;PREXASERTIB;5-((5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile;5-[[5-[2-(3-Aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]-2-pyrazinecarbonitrile;2-Pyrazinecarbonitrile, 5-[[5-[2-(3-aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]-
CBNumber
CB82667926
Molecular Formula
C18H19N7O2
Formula Weight
365.39
MOL File
1234015-52-1.mol
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LY 2606368 Property

Boiling point:
608.5±55.0 °C(Predicted)
Density 
1.37±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
insoluble in DMSO
form 
A crystalline solid
pka
11.89±0.10(Predicted)
color 
Light yellow to brown
InChI
InChI=1S/C18H19N7O2/c1-26-14-4-2-5-15(27-7-3-6-19)18(14)13-8-16(25-24-13)23-17-11-21-12(9-20)10-22-17/h2,4-5,8,10-11H,3,6-7,19H2,1H3,(H2,22,23,24,25)
InChIKey
DOTGPNHGTYJDEP-UHFFFAOYSA-N
SMILES
C1(C#N)=NC=C(NC2C=C(C3=C(OC)C=CC=C3OCCCN)NN=2)N=C1
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

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

Cayman Chemical
Product number
21490
Product name
LY2606368
Purity
≥98%
Packaging
1mg
Price
$116
Updated
2024/03/01
Cayman Chemical
Product number
21490
Product name
LY2606368
Purity
≥98%
Packaging
5mg
Price
$486
Updated
2024/03/01
Cayman Chemical
Product number
21490
Product name
LY2606368
Purity
≥98%
Packaging
10mg
Price
$799
Updated
2024/03/01
Cayman Chemical
Product number
21490
Product name
LY2606368
Purity
≥98%
Packaging
25mg
Price
$1141
Updated
2024/03/01
Usbiological
Product number
454002
Product name
LY 2606368
Packaging
500ug
Price
$566
Updated
2021/12/16
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LY 2606368 Chemical Properties,Usage,Production

Description

LY2606368 is a checkpoint kinase 1 (Chk1) inhibitor with a Ki value of 0.9 nM against the purified target and IC50 values of <13 nM in a viability study of multiple colorectal cancer cell lines. Inhibition of Chk1 causes double-strand DNA breakage in cells leading to an excessive cell damage burden and subsequent cell death. In vitro, LY2606368 inhibits the doxorubicin-activated G2/M checkpoint in p53-deficient HeLa cells with an EC50 value of 9 nM. LY2606368, at 25 nM, also significantly induces apoptosis and inhibits colony formation in AGS and MKN1 gastric cancer cells.

Uses

LY 2606368 is a novel CHK1 inhibitor under investigation as a chemopotentiating agent. It causes double-stranded DNA breakage while simultaneously removing the protection of the DNA damage checkpoints. LY 2606368 is representative of a novel class of drugs for the treatment of cancer and tumor growth inhibition.

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)[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.

IC 50

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

References

[1] wu w, bi c, bence a k, et al. antitumor activity of chk1 inhibitor ly2606368 as a single agent in sw1990 human pancreas orthotopic tumor model. cancer research, 2012, 72(8 supplement): 1776.
[2] lainchbury m, matthews t p, mchardy t, et al. discovery of 3-alkoxyamino-5-(pyridin-2-ylamino) pyrazine-2-carbonitriles as selective, orally bioavailable chk1 inhibitors. journal of medicinal chemistry, 2012, 55(22): 10229-10240.
[3] mcneely s c, burke t f, durlandbusbice s, et al. abstract a108: ly2606368, a second generation chk1 inhibitor, inhibits growth of ovarian carcinoma xenografts either as monotherapy or in combination with standard-of-care agents. molecular cancer therapeutics, 2011, 10(supplement 1): a108.

LY 2606368 Preparation Products And Raw materials

Raw materials

Preparation Products

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LY 2606368 Suppliers

China 94 United States 10 Global 104
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4769
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55
Heze Development Zone chuangli Chemical Co., Ltd.
Tel
0530-+86-530-529 6766，+86-15666160102 15666160102
Fax
0530-529 6766
Email
info@chuangli-chem.com
Country
China
ProdList
836
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55
Shanghai Easy CDMO Co.,Ltd
Tel
021-61734564 13854185395;
Email
info@easycdmo.com
Country
China
ProdList
10024
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
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58
CEG Chemical Science&Technology Co., Ltd.
Tel
Mobile:13665161512
Fax
+86-510-68873513
Country
China
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1785
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AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
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2990
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60
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
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58
Shanghai YuanQi Biotechnology Co., Ltd.
Tel
+86-2332782371 +86-18120098618
Email
sales@adobechem.com
Country
China
ProdList
1250
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50

1234015-52-1, LY 2606368Related Search:

LY 294002 Hydrochloride 1-[5-ETHYL-2-HYDROXY-4-[[6-METHYL-6-(1H-TETRAZOL-5-YL)HEPTYL]OXY]PHENYL]ETHANONE LY-404039 LY3143921 LY 379268 LY-2940094 LY2109761 LY 2784544

  • LY 2606368
  • 5-((5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile LY2606368
  • 5-[[5-[2-(3-Aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]-2-pyrazinecarbonitrile
  • 5-((5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile
  • Prexasertib
  • LY 2606368;LY-2606368;PREXASERTIB
  • Prexasertib (LY2606368)
  • CS-1453
  • 2-Pyrazinecarbonitrile, 5-[[5-[2-(3-aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]-
  • Prexasertib free base
  • SIK,Prexasertib,LY 2606368,Checkpoint Kinase (Chk),HT-29,S296,Apoptosis,DNA,double-stranded,inhibit,autophosphorylation,H2AX,ATP-competitive,HeLa,MELK,RSK1,CDK2,LY-2606368,Inhibitor,S516,ARK5,replication,BRSK2,CDC25A
  • LY2606368 HCl(free base)
  • 1234015-52-1
  • C18H19N7O2