ChemicalBook--->CAS DataBase List--->396129-53-6

396129-53-6

396129-53-6 Structure

396129-53-6 Structure
IdentificationBack Directory
[Name]

LY-364947
[CAS]

396129-53-6
[Synonyms]

CS-576
Y364947
E 616451
LY-364947
HTS 466284
LY-364947, >=98%
LY 364947;LY-364947
LY-364947 USP/EP/BP
LY364947(HTS 466284)
LY-364947, 396129-53-6
TGF-β RI Kinase Inhibitor
LY-364947?,HTS 466284, >98%
LY 364947;LY364947;HTS466284
LY364947;HTS466284; LY-364947
[3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole
4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline
Quinoline, 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-
4-[(3-Pyridin-2-yl)-1H-pyrazol-4-yl)]quinoline 95+%
TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem
Transforming Growth Factor-β Type I Receptor Kinase Inhibitor
LY 364947 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]quinoline
2-[4-(Quinolin-4-yl)-1H-pyrazol-3-yl]pyridine, 3-(Pyridin-2-yl)-4-(quinolin-4-yl)-1H-pyrazole
4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]quinoline E 616451
[Molecular Formula]

C17H12N4
[MDL Number]

MFCD00800758
[MOL File]

396129-53-6.mol
[Molecular Weight]

272.31
Chemical PropertiesBack Directory
[Melting point ]

>230℃ (dec.)
[Boiling point ]

490.8±45.0 °C(Predicted)
[density ]

1.283±0.06 g/cm3(Predicted)
[storage temp. ]

Store at RT
[solubility ]

DMSO: soluble2mg/mL, clear
[form ]

powder
[pka]

8.94±0.50(Predicted)
[color ]

white to beige
[Stability:]

Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
[InChIKey]

IBCXZJCWDGCXQT-UHFFFAOYSA-N
Safety DataBack Directory
[Hazard Codes ]

T,N
[Risk Statements ]

25-36/37/38-50/53
[Safety Statements ]

26-45-60-61
[RIDADR ]

UN 2811 6.1/PG 3
[WGK Germany ]

3
[HS Code ]

2933491090
Hazard InformationBack Directory
[Description]

LY-364947 (396129-53-6) is a selective ALK5 inhibitor, IC50 = 59, 400 and 1400 nM for TGF-β RI, TGF-β RII and MLK-7K, respectively.1 Inhibits Smad2 phosphorylation induced by TGF-β as well as fibronectin expression and MDA-MB-231 cell invasion.2 LY-364947 abolishes resistance of glioblastoma-initiating cells to radiation.3?Cell permeable.
[Uses]

Cell permeable, potent, selective and ATP-competitive inhibitor of TGF-β RI kinase (IC50=51nM). Displays ~15-fold greater selectivity over p38α MAPK (IC50=740nM). Inhibits TGF-β-dependent cellular growth (IC50=89nM in NIH 3T3 mouse fibroblasts) and transcription activation (IC50=47nM in mink lung cells). Suppresses invasion of MDA-MB-231 breast cancer cells in a matrigel invasion assay.
[Definition]

ChEBI: LY 364947 is a member of the class of pyrazoles carrying pyridin-2-yl and quinolin-4-yl substituents at positions 3 and 4 respectively. It has a role as a TGFbeta receptor antagonist. It is a member of pyrazoles, a member of pyridines and a member of quinolines.
[Biological Activity]

Selective inhibitor of TGF- β type-I receptor (TGF- β RI, TGFR-I, T β R-I, ALK-5) (IC 50 values are 59, 400 and 1400 nM for TGR- β RI, TGF- β RII and MLK-7K respectively). Inhibits TGF- β -dependent luciferase production in mink lung cells (p3TP lux) and growth in mouse fibroblasts (NIH 3T3) (IC 50 values are 47 and 89 nM respectively). Suppresses invasion of MDA-MB-231 breast cancer cells in a matrigel invasion assay.
[Biochem/physiol Actions]

LY-364947 is a selective, ATP-competitive inhibitor of Transforming Growth Factor-β Type I receptor kinase (TGF-β RI, ALK5) with IC50 = 59 nM. It is much less potent at related kinases, with IC50 = 400 nM for TGF-β RII and IC50 = 1400 nM for mixed lineage kinase-7 (MLK-7), a kinase in the MAP kinase signal pathway and closely related to TGF-β RII. LY-364947 inhibits TGF-β-dependent cellular growth (IC50 = 81 nM) in NIH 3T3 mouse fibroblasts.
[in vitro]

ly364947 was quickly identified as a potent inhibitor (ic50= 51 nm) and was chosen as a platform for sar development. compounds were further evaluated as inhibitors of tgf-β-dependent luciferase production in mink lung cells (p3tp lux) and growth in mouse fibroblasts (nih 3t3) [1].
[in vivo]

in a rat model of nmda-induced retinal degeneration, simultaneous injection of nmda and the tgf-β inhibitor ly364947 slightly but significantly attenuated the reduction in number of cells in the ganglion cell layer and almost completely prevented the enhancement of capillary degeneration. [3].
[storage]

Store at RT
[References]

1) Sawyer?et al. (2003),?Synthesis and activity of new aryl-and hetero-aryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain; J. Med. Chem.,?46?3953 2) Shiou?et al. (2006),?Smad4-dependent regulation of urokinase plasminogen activator secretion and RNA stability associated with invasiveness by autocrine and paracrine transforming growth factor-beta; J. Biol. Chem.,?281?33971 3) Hardee?et al. (2012),?Resistance of glioblastoma-initiating cells to radiation mediated by the tumor microenvironment can be abolished by inhibiting transforming growth factor-β; Cancer Res.,?72?4119
Spectrum DetailBack Directory
[Spectrum Detail]

LY-364947(396129-53-6)1HNMR
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