LY-364947

ChemicalBook > CAS DataBase List > LY-364947

Product Name: LY-364947
CAS No.: 396129-53-6
Chemical Name: LY-364947
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
CBNumber: CB3972214
Molecular Formula: C17H12N4
Formula Weight: 272.3
MOL File: 396129-53-6.mol

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LY-364947 Property

Melting point:: >230℃ (dec.)
Boiling point:: 490.8±45.0 °C(Predicted)
Density: 1.283±0.06 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: DMSO: soluble2mg/mL, clear
pka: 8.94±0.50(Predicted)
form: powder
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

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Safety

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

H400Very toxic to aquatic life

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P273Avoid release to the environment.

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: L6293
Product name: LY-364947
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $209
Updated: 2024/03/01

Sigma-Aldrich

Product number: 616451-M
Product name: TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem
Packaging: 616451-5UNMG
Price: $18700
Updated: 2024/03/01

Sigma-Aldrich

Product number: 616451-M
Product name: TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem
Packaging: 616451-5MG
Price: $189
Updated: 2023/06/20

Cayman Chemical

Product number: 13341
Product name: LY364947
Purity: ≥98%
Packaging: 5mg
Price: $92
Updated: 2024/03/01

Cayman Chemical

Product number: 13341
Product name: LY364947
Purity: ≥98%
Packaging: 10mg
Price: $174
Updated: 2024/03/01

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LY-364947 Chemical Properties,Usage,Production

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

LY 364947, is a potent ATP-competitive inhibitor of Tgf-b signaling.

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

LY-364947 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from LY-364947 manufacturers

Wuhan Nutra Biotechnology Co.,Ltd

Product: LY-364947 396129-53-6
Price: US $0.00-0.00/g
Min. Order: 1g
Purity: 98%
Supply Ability: 1000kgs
Release date: 2021-05-24

Career Henan Chemical Co

Product: LY-364947 396129-53-6
Price: US $1.00/KG
Min. Order: 1KG
Purity: 98%
Supply Ability: 20kg
Release date: 2019-09-05

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[3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole

4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline

LY364947(HTS 466284)

E 616451

HTS 466284

2-[4-(Quinolin-4-yl)-1H-pyrazol-3-yl]pyridine, 3-(Pyridin-2-yl)-4-(quinolin-4-yl)-1H-pyrazole

Quinoline, 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-

4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]quinoline E 616451

LY 364947 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]quinoline

LY-364947, 396129-53-6

Transforming Growth Factor-β Type I Receptor Kinase Inhibitor

LY-364947

LY-364947, >=98%

LY364947;HTS466284; LY-364947

TGF-β RI Kinase Inhibitor

CS-576

LY 364947;LY-364947

LY-364947?,HTS 466284, >98%

TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem

4-[(3-Pyridin-2-yl)-1H-pyrazol-4-yl)]quinoline 95+%

LY 364947;LY364947;HTS466284

Y364947

LY-364947 USP/EP/BP

LY-364947 LY364947 TGF-β RI Kinase Inhibitor

396129-53-6

6129-53-6

C17H12N4

API

Inhibitors

Smad

TGF-beta