911222-45-2

Name	LY2603618
Synonyms	IC-83 CS-508 LY2603618 RABUSERTIB LY-2603618 LY 2603618 ly2603618 IC-83 3-(5-BroMo-4-Methyl-2-[(2s)-Morpholin-2- N-[5-Bromo-4-methyl-2-[(2S)-2-morpholinylmethoxy]phenyl]-N'-(5-methyl-2-pyrazinyl)urea
CAS	911222-45-2

Molecular Formula	C18H22BrN5O3
Molar Mass	436.3
Density	1.461
Boling Point	503.1±50.0 °C(Predicted)
Solubility	Soluble in water (<1 mg/ml) at 25 °C, DMSO (13 mg/ml) at 25 °C, and ethanol (<1 mg/
Appearance	solid
Color	Off-white
pKa	12.06±0.70(Predicted)
Storage Condition	-20°C
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.
Use	A selective Chk1 inhibitor.
In vitro study	Chk 1 is an ATP-dependent threonine protein kinase and a key protein in the double-strand break (DSBs)-initiated DNA replication checkpoint system. Chk 1 is involved in all currently proven cell cycle checkpoints, including G1/S, S-phase, G 2 /M, and mitotic spindle checkpoints. LY2603618 can interfere with the repair of DNA damage caused by biochemical reagents by inhibiting Chk 1 activity, thereby enhancing the anti-tumor efficacy of various chemotherapeutic drugs. However, no clinical trials have been reported. Inhibition of Chk 1 enhances the effects of antimetabolites, such as gemcitabine. LY2603618 treatment impairs DNA synthesis, increases DNA damage (through defects in cell division), and induces apoptosis. It can be used in conjunction with pemetrexed, especially for tumor cells with p53 mutations.
In vivo study	In xenograft models, LY2603618 can be used in combination with pemetrexed to inhibit tumor growth.

HS Code

29349990

Y2603618 is a selective Chk1 inhibitor with potential antitumor activity. Phase 2.

Last Update：2022-10-16 17:41:52

biological activity	LY2603618 is a selective Chk1 inhibitor with potential anti-tumor activity. Phase 2. Rabusertib (LY2603618, IC-83) is a highly selective Chk1 inhibitor with potential anti-tumor activity in cell-free tests, IC50 = 7 nM, and its efficacy on Chk1 is more than 100 times higher than that of other detected protein kinases. Rabusertib (LY2603618) can induce cell cycle arrest, DNA damage response and autophagy in cancer cells. Rabusertib (LY2603618) induces bak-dependent apoptosis in AML cell lines.
Target	Value
Chk1 (Cell-free assay)	7 nM

Last Update：2024-04-09 02:00:08

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Product Name: Rabusertib Request for quotation
CAS: 911222-45-2
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052

Wechat: 15671228036

Product Name: LY2603618 Visit Supplier Webpage Request for quotation
CAS: 911222-45-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

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911222-45-2

911222-45-2 Request for Quotation