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;Prexasertib 2HCl;LY 2606368;LY-2606368;LY-2606368 (Prexasertib);LY-2606368 dihydrochloride;Prexasertib dihydrochloride;Prexasertib HCl (LY2606368);Prexasertib (LY2606368) 2HCl
- CBNumber:
- CB02669661
- Molecular Formula:
- C18H21Cl2N7O2
- Molecular Weight:
- 438.31104
- MDL Number:
- MOL File:
- 1234015-54-3.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| Prexasertib HCl (LY2606368) | JZB01554 | 25mg | $1190 |
| Prexasertib HCl (LY2606368) | JZB01554 | 50mg | $1655 |
| Prexasertib HCl (LY2606368) | JZB01554 | 100mg | $2647 |
| Prexasertib dihydrochloride 99.42% | CS-3507 | 5mg | $119 |
| Prexasertib dihydrochloride 99.42% | CS-3507 | 10mg | $195 |
| More product size | |||
5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile hydrochloride Properties
| 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 |
| FDA UNII | 9RFT476U2L |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile hydrochloride price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Biosynth | JZB01554 | Prexasertib HCl (LY2606368) | 1234015-54-3 | 25mg | $1190 | 2026-06-04 | Buy |
| Biosynth | JZB01554 | Prexasertib HCl (LY2606368) | 1234015-54-3 | 50mg | $1655 | 2026-06-04 | Buy |
| Biosynth | JZB01554 | Prexasertib HCl (LY2606368) | 1234015-54-3 | 100mg | $2647 | 2026-06-04 | Buy |
| ChemScene | CS-3507 | Prexasertib dihydrochloride 99.42% | 1234015-54-3 | 5mg | $119 | 2026-06-04 | Buy |
| ChemScene | CS-3507 | Prexasertib dihydrochloride 99.42% | 1234015-54-3 | 10mg | $195 | 2026-06-04 | Buy |
5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile hydrochloride Chemical Properties,Uses,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
| 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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19936 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32466 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471; | sales@sarms4muscle.com | China | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49734 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3135 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39039 | 58 |
| Chemtour Biotech Co., Ltd | +8617327281506 | market@chemtour.com | China | 1521 | 58 |
View Lastest Price from 5-(5-(2-(3-aMinopropoxy)-6-Methoxyphenyl)-1H-pyrazol-3-ylaMino)pyrazine-2-carbonitrile hydrochloride manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2026-06-02 | Prexasertib dihydrochloride
1234015-54-3
|
$38.00-89.00 | 98.46% | 10g | TargetMol Chemicals Inc. |
-
- Prexasertib dihydrochloride
1234015-54-3
- $38.00-89.00
- 98.46%
- TargetMol Chemicals Inc.
