LY2603618
Description In vitro In vivo- Product Name
- LY2603618
- CAS No.
- 911222-45-2
- Chemical Name
- LY2603618
- Synonyms
- IC-83;CS-508;LY2603618;Rabusertib;ly2603618 IC-83;RABUSERTIB;IC-83;LY2603618, >=99%;Rabusertib (LY2603618);ly2603618 IC-83 USP/EP/BP;IC-83; LY 2603618; LY-2603618
- CBNumber
- CB92538917
- Molecular Formula
- C18H22BrN5O3
- Formula Weight
- 436.3
- MOL File
- 911222-45-2.mol
LY2603618 Property
- Boiling point:
- 503.1±50.0 °C(Predicted)
- Density
- 1.461
- storage temp.
- -20°C
- solubility
- Soluble in DMSO (up to 10 mg/ml)
- pka
- 12.06±0.70(Predicted)
- form
- solid
- color
- Off-white
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Safety
- HS Code
- 29349990
N-Bromosuccinimide Price
- Product number
- 20351
- Product name
- LY2603618
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $40
- Updated
- 2024/03/01
- Product number
- 20351
- Product name
- LY2603618
- Purity
- ≥95%
- Packaging
- 50 mg
- Price
- $236
- Updated
- 2024/03/01
- Product number
- 20351
- Product name
- LY2603618
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2022/04/27
- Product number
- 20351
- Product name
- LY2603618
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $72
- Updated
- 2024/03/01
- Product number
- 20351
- Product name
- LY2603618
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $158
- Updated
- 2024/03/01
LY2603618 Chemical Properties,Usage,Production
Description
LY2603618 is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated.
In vitro
Chk1 is an ATP-dependent serine-threonine kinase and a key component in the DNA replication-monitoring checkpoint system activated by double-stranded breaks (DSBs). Chk1 contributes to all currently defined cell cycle checkpoints, including G1/S, intra-S-phase, G2/M, and the mitotic spindle checkpoint. By inhibiting the activity of chk1, LY2603618 prevents the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. However, preclinical data involving LY2603618 has not been published until now. Inhibition of Chk1 is predicted to enhance the effects of antimetabolites, such as gemcitabine. LY2603618 treatment impairs DNA synthesis, increases DNA damage (via mitotic defects), induces apoptosis, and has synergistic activity with pemetrexed, especially in p53 mutant tumor cells.
In vivo
In xenograft models, LY2603618 delays tumor growth when given in combination with pemetrexed.
Description
LY2603618 (911222-45-2) is a potent (IC50?= 7nM) and selective (>1000x over Chk2) Checkpoint kinase 1 (Chk1) inhibitor.1?Chk1 is an important regulator of the DNA damage response – combination treatment of LY2603618 with other chemotherapeutic agents significantly increased tumor growth inhibition when compared to chemotherapeutic alone.2,3,4?LY2603618 caused a dramatic suppression of cell growth in MCF-7 and MDA-MB-231 human breast cancer cells?via?Chk1 inhibition induced upregulation of replication stress caused by oncogenes.5
Uses
LY2603618 is a selective Chk1 inhibitor that can treat idiopathic pulmonary fibrosis.
Definition
ChEBI: 1-[5-bromo-4-methyl-2-[[(2S)-2-morpholinyl]methoxy]phenyl]-3-(5-methyl-2-pyrazinyl)urea is a member of ureas.
Biological Activity
Rabusertib (LY2603618, IC-83) is a highly selective inhibitor of Chk1 with potential antitumor activity in cell-free assays, IC50=7 nM, potency against Chk1 versus multiple other protein kinases tested 100 times higher. Rabusertib (LY2603618) induces cell cycle arrest, DNA damage response and autophagy in cancer cells. Rabusertib (LY2603618) induces bak-dependent apoptosis in AML cell lines.
in vivo
experiment was carried out to determine the combining effect of ly2603618 with other chemotherapy[2] . in mice xenograft model that inculated with calu-6 lung cancer cell, combining administration of injected gemcitabine 150 mg/kg and orally uptake ly2603618 (200 mg/kg) resulted in increased dna damage of tumour, as was demonstrated by a 2-fold increase in chk1 s345 phosphorylation in comparison with mice treated with gemcitabine alone[2].
storage
Store at -20°C
References
1) King?et al.?(2014),?Characterization and preclinical development of LY2603618: a selective and potent Chk1 inhibitor; Invest. New Drugs,?32?213 2) Calvo?et al.?(2014),?Preclinical analyses and phase I evaluation of LY2603618 administered in combination with pemetrexed and cisplatin in patients with advanced cancer; Invest. New Drugs,?32?955 3) Calvo?et al. (2016),?Phase I Study of CHK1 Inhibitor LY2603618 in Combination with Gemcitabine in Patients with Solid Tumors; Oncology,?91?251 4) Zhao?et al.?(2016),?Inhibition of CHK1 enhances cell death induced by the Bcl-1-selective inhibitor ABT-199 in acute myeloid leukemia cells; Oncotarget,?7?34785 5) Zhang?et al.?(2016),?Targeting radioresistant breast cancer cells by single agent CHK1 inhibitor via enhancing replication stress; Oncotarget,?7?34688
LY2603618 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from LY2603618 manufacturers
- Product
- ly2603618 IC-83 911222-45-2
- Price
- US $9.80/KG
- Min. Order
- 1g
- Purity
- ≥99%
- Supply Ability
- 100kg
- Release date
- 2019-12-25