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Merck
모든 사진(1)

주요 문서

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SML2567

Sigma-Aldrich

LY2784544

≥98% (HPLC)

동의어(들):

3-(4-Chloro-2-fluorobenzyl)-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine, 3-[(4-Chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)imidazo[1,2-b]pyridazin-6-amine, LY 2784544, LY-2784544

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모든 사진(1)

About This Item

실험식(Hill 표기법):
C23H25ClFN7O
CAS Number:
1229236-86-5
Molecular Weight:
469.94
MDL number:
MFCD20482143
UNSPSC 코드:
12352200
NACRES:
NA.77

분석

≥98% (HPLC)

형태

powder

구성

H2O, 0-4 mol/mol (moles per mole of product)

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

2-8°C

InChI

1S/C23H25ClFN7O/c1-14-9-21(29-28-14)27-22-11-17(13-31-5-7-33-8-6-31)23-26-15(2)20(32(23)30-22)10-16-3-4-18(24)12-19(16)25/h3-4,9,11-12H,5-8,10,13H2,1-2H3,(H2,27,28,29,30)

InChI key

SQSZANZGUXWJEA-UHFFFAOYSA-N

생화학적/생리학적 작용

LY2784544 is an orally active, ATP-competitive, potent and JAK2-selective janus tyrosine kinase inhibitor (IC50/[ATP] = 2.52 nM/5 μM/JAK2, 19.8 nM/20 μM/JAK1, 48.0 nM/2 μM/JAK3) with little activity toward 79 other kinases. LY2784544 selectively inhibits signaling/proliferation driven by oncogenic JAK2V617F (IC50 = 20/55 nM) over those mediated by wt JAK2 upon IL-3 induction (IC50 = 1183/1309 nM) in Ba/F3 cultures and displays in vivo efficacious in a JAK2V617F-induced murine MPN model (10-80 mg/kg bid po.). LY2784544 is also reported to display Zn-dependent (optimal [Zn+2] = 100 μM) GPR39 agonist activity, but not 11 other GPRs.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

시험 성적서(COA)

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Nuramalina H Mumin et al.
BMC cancer, 19(1), 102-102 (2019-01-27)
Due to the lack of effective therapies and poor prognosis in TNBC (triple-negative breast cancer) patients, there is a strong need to develop effective novel targeted therapies for this subtype of breast cancer. Inhibition of heat shock protein 90 (HSP90)
L Ma et al.
Blood cancer journal, 3, e109-e109 (2013-04-16)
Owing to the prevalence of the JAK2V617F mutation in myeloproliferative neoplasms (MPNs), its constitutive activity, and ability to recapitulate the MPN phenotype in mouse models, JAK2V617F kinase is an attractive therapeutic target. We report the discovery and initial characterization of
Wei Zhou et al.
Oncogene, 37(29), 3981-3997 (2018-04-18)
Antineoplastic platinum agents are used in first-line treatment of ovarian cancer, but treatment failure frequently results from platinum drug resistance. Emerging observations suggest a role of reactive oxygen species (ROS) in the resistance of cancer drugs including platinum drugs. However
Seiji Sato et al.
Molecular pharmacology, 90(6), 726-737 (2016-11-03)
In this study, we identified two previously described kinase inhibitors-3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(3-methyl-1H-pyrazol-5-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine (LY2784544) and 1H-benzimidazole-4-carboxylic acid, 2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(4-morpholinyl)- (GSK2636771)-as novel GPR39 agonists by unbiased small-molecule-based screening using a β-arrestin recruitment screening approach (PRESTO-Tango). We characterized the signaling of LY2784544 and GSK2636771 and compared
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