ChemicalBook >> CAS DataBase List >>LY-364947

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
Molecular Weight:
272.3
MDL Number:
MFCD00800758
MOL File:
396129-53-6.mol
MSDS File:
SDS
Last updated:2023-06-30 15:45:59

LY-364947 Properties

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

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictogramsGHS hazard pictograms
GHS06,GHS09
Signal word  Danger
Hazard statements  H301-H315-H319-H335-H400
Precautionary statements  P261-P273-P301+P310-P305+P351+P338
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
NFPA 704
0
2 0

LY-364947 price More Price(38)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich L6293 LY-364947 ≥98% (HPLC) 396129-53-6 5mg $209 2024-03-01 Buy
Sigma-Aldrich 616451-M TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem 396129-53-6 616451-5UNMG $18700 2024-03-01 Buy
Sigma-Aldrich 616451-M TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem 396129-53-6 616451-5MG $189 2023-06-20 Buy
Cayman Chemical 13341 LY364947 ≥98% 396129-53-6 5mg $92 2024-03-01 Buy
Cayman Chemical 13341 LY364947 ≥98% 396129-53-6 10mg $174 2024-03-01 Buy
Product number Packaging Price Buy
L6293 5mg $209 Buy
616451-M 616451-5UNMG $18700 Buy
616451-M 616451-5MG $189 Buy
13341 5mg $92 Buy
13341 10mg $174 Buy

LY-364947 Chemical Properties,Uses,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

2459-07-6
396129-53-6
Synthesis of LY-364947 from Methyl picolinate

LY-364947 Preparation Products And Raw materials

Global( 140)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32480 60
career henan chemical co
+86-0371-86658258 sales@coreychem.com China 29914 58
Hubei Jusheng Technology Co.,Ltd.
18871490254 linda@hubeijusheng.com CHINA 28180 58
Alchem Pharmtech,Inc.
8485655694 sales@alchempharmtech.com United States 63711 58
SHANGHAI T&W PHARMACEUTICAL CO., LTD.
+86-021-61551413 +8618813727289 contact@trustwe.com China 5739 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 19892 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250 1026@dideu.com China 29831 58
Wuhan Nutra Biotechnology Co.,Ltd
+8617786394783 nutrabiotech@outlook.com China 300 58
Zhejiang J&C Biological Technology Co.,Limited
+1-2135480471 +1-2135480471 sales@sarms4muscle.com China 10523 58
InvivoChem
+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6393 58

View Lastest Price from LY-364947 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
LY-364947 pictures 2021-10-08 LY-364947
396129-53-6
US $0.00-0.00 / g 1g 98% 1000kgs Wuhan Nutra Biotechnology Co.,Ltd
LY-364947 pictures 2019-09-06 LY-364947
396129-53-6
US $1.00 / KG 1KG 98% 20kg Career Henan Chemical Co
  • LY-364947 pictures
  • LY-364947
    396129-53-6
  • US $0.00-0.00 / g
  • 98%
  • Wuhan Nutra Biotechnology Co.,Ltd
  • LY-364947 pictures
  • LY-364947
    396129-53-6
  • US $1.00 / KG
  • 98%
  • Career Henan Chemical Co

LY-364947 Spectrum

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 [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 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