Rabusertib (LY2603618) - Moligand™, 10mM in DMSO , Serine/threonine-protein kinase Chk1 inhibitor, CAS No.911222-45-2, Serine/threonine-protein kinase Chk1 inhibitor

CAS: 911222-45-2 Cat. No.: R408734 Formula: C₁₈H₂₂BrN₅O₃ Peso molecolare: 436.3

QUALITÀ & PUREZZA Moligand™, 10mM in DMSO

Synonyms

IC-83 | (S)-1-(5-bromo-4-methyl-2-(morpholin-2-ylmethoxy)phenyl)-3-(5-methylpyrazin-2-yl)urea

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

Information

Rabusertib (LY2603618, IC-83) is a highly selectiveChk1inhibitor 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. Rabuserti
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.
Cell Data

cell lines：

Concentrations：5 or 10 μM

Incubation Time：24 h

Powder Purity:≥97%

Specifiche

Sinonimi

IC-83 | (S)-1-(5-bromo-4-methyl-2-(morpholin-2-ylmethoxy)phenyl)-3-(5-methylpyrazin-2-yl)urea

Specifiche e purezza

Moligand™, 10mM in DMSO

Meccanismi biochimici e fisiologici

Rabusertib (LY2603618, IC-83) 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. Rabuser

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Grado

Moligand™

Tipo di azione

INHIBITOR

Meccanismo d'azione

Serine/threonine-protein kinase Chk1 inhibitor

Proprietà del prodotto

ALogP

1.4

Nomi e identificatori

Isomeri SMILES

CC1=CC(=C(C=C1Br)NC(=O)NC2=NC=C(N=C2)C)OC[C@@H]3CNCCO3

Peso molecolare

436.3

Reaxy-Rn

39808750

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=39808750&ln=

Obiettivi associati (umani)

CHEK1 Tchem Serine/threonine-protein kinase Chk1 (2 Activities)

Discover Target: CHEK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Proprietà chimiche e fisiche

• Solubilità: Solubility (25°C) In vitro DMSO: 48 mg/mL (197.28 mM); Ethanol: 48 mg/mL (197.28 mM); Water: Insoluble