LY 2606368
- CAS No.
- 1234015-52-1
- Chemical Name:
- LY 2606368
- Synonyms
- Prexasertib;CS-1453;LY 2606368;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
- Molecular Weight:
- 365.39
- MDL Number:
- MFCD25977016
- MOL File:
- 1234015-52-1.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| 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 |
| FDA UNII | 820NH671E6 |
| NCI Drug Dictionary | prexasertib |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
LY 2606368 price More Price(45)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 21490 | LY2606368 ≥98% | 1234015-52-1 | 1mg | $32 | 2026-04-30 | Buy |
| Cayman Chemical | 21490 | LY2606368 ≥98% | 1234015-52-1 | 5mg | $104 | 2026-04-30 | Buy |
| Cayman Chemical | 21490 | LY2606368 ≥98% | 1234015-52-1 | 10mg | $160 | 2026-04-30 | Buy |
| Cayman Chemical | 21490 | LY2606368 ≥98% | 1234015-52-1 | 25mg | $280 | 2026-04-30 | Buy |
| Biosynth | FA161375 | LY2606368 | 1234015-52-1 | 1mg | $250 | 2026-06-04 | Buy |
LY 2606368 Chemical Properties, Uses, 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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Heze Development Zone chuangli Chemical Co., Ltd. | 0530-+86-530-529 6766，+86-15666160102 15666160102 | info@chuangli-chem.com | China | 849 | 55 |
| Shandong Dayou Pharmaceutical Research and Development Co., Ltd. | hanfangpharma@126.com 15165037910 | hanfangpharma@126.com | China | 25800 | 58 |
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2915 | 55 | |
| Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7545 | 61 |
| MedChemexpress LLC | 021-58955995 | sales@medchemexpress.cn | United States | 4853 | 58 |
| Guangzhou Isun Pharmaceutical Co., Ltd | 020-39119399 18927568969 | isunpharm@qq.com | China | 4773 | 55 |
| CEG Chemical Science&Technology Co., Ltd. | Mobile:13665161512 | China | 1784 | 58 | |
| Bide Pharmatech Ltd. | 400-164-7117 18317119277 | product02@bidepharm.com | China | 40000 | 60 |
| AdooQ Bioscience CHINA | 025-58849295 | info@adooq.cn | China | 2981 | 60 |
| LETOPHARM LIMITED | +86-21-5821 5861 | sales@letopharm.com | China | 2374 | 58 |
