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Merck

SML2855

Sigma-Aldrich

LY2603618

≥98% (HPLC)

Sinónimos:

(S)-1-[5-Bromo-4-methyl-2-(morpholin-2-ylmethoxy)phenyl]-3-(5-methylpyrazin-2-yl)urea, 1-[5-Bromo-4-methyl-2-(S)-(morpholin-2-ylmethoxy)phenyl]-3-(5-methylpyrazin-2-yl)urea, IC-83, LCI-1, LY 2603618, LY-2603618, Rabusertib

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About This Item

Fórmula empírica (notación de Hill):
C18H22BrN5O3
Número de CAS:
Peso molecular:
436.30
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77

Nivel de calidad

Ensayo

≥98% (HPLC)

Formulario

powder

color

white to beige

solubilidad

DMSO: 2 mg/mL, clear (warmed)

temp. de almacenamiento

2-8°C

cadena SMILES

CC1=C(Br)C=C(NC(NC2=CN=C(C)C=N2)=O)C(OC[C@H]3OCCNC3)=C1

InChI

1S/C18H22BrN5O3/c1-11-5-16(27-10-13-8-20-3-4-26-13)15(6-14(11)19)23-18(25)24-17-9-21-12(2)7-22-17/h5-7,9,13,20H,3-4,8,10H2,1-2H3,(H2,22,23,24,25)/t13-/m0/s1

Clave InChI

SYYBDNPGDKKJDU-ZDUSSCGKSA-N

Acciones bioquímicas o fisiológicas

LY2603618 (LCI-1) is a potent and selective checkpoint kinase 1 (Chk1) inhibitor (IC50 = 7 nM) that produces a cellular phenotype identical to that reported upon Chk1 depletion by RNAi. LY2603618 prevents doxorubicin-induced Chk1 autophosphorylation (IC50 = 52 nM; HeLa), allowing cells to traverse the G2/M checkpoint and proceed into mitosis with unresolved replicated chromosomes. LY2603618 renders mutant p53, but not wild-type, HT-29 colon cancer cells more sensitive to gemcitabine both in vitro and in mice in vivo.

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


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Investigational new drugs, 32(2), 213-226 (2013-10-12)
Interference with DNA damage checkpoints has been demonstrated preclinically to be a highly effective means of increasing the cytotoxicity of a number of DNA-damaging cancer therapies. Cell cycle arrest at these checkpoints protects injured cells from apoptotic cell death until
Nicole D Vincelette et al.
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CPX-351 is a liposomally encapsulated 5:1 molar ratio of cytarabine and daunorubicin that recently received regulatory approval for the treatment of therapy-related acute myeloid leukemia (AML) or AML with myelodysplasia-related changes based on improved overall survival compared to standard cytarabine/daunorubicin
Characterization and preclinical development of LCI-1, a selective and potent Chk1 inhibitor in phase I clinical trials
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Molecular Cancer Therapeutics, 8, B248-B248 (2009)
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The EMBO journal, 38(20), e101443-e101443 (2019-08-20)
Cyclins are central engines of cell cycle progression in conjunction with cyclin-dependent kinases (CDKs). Among the different cyclins controlling cell cycle progression, cyclin F does not partner with a CDK, but instead forms via its F-box domain an SCF (Skp1-Cul1-F-box)-type

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