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
| 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) |   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 |
|
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 |
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
LY-364947 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32957 | 60 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | sales@coreychem.com | China | 29882 | 58 |
| Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28172 | 58 |
| Alchem Pharmtech,Inc. | 8485655694 | sales@alchempharmtech.com | United States | 63687 | 58 |
| SHANGHAI T&W PHARMACEUTICAL CO., LTD. | +86-021-61551413 +8618813727289 | contact@trustwe.com | China | 5738 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32165 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 22883 | 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 | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
View Lastest Price from LY-364947 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-11-19 | LY-364947
396129-53-6
|
US $59.00-146.00 / mg | 99.96% | 10g | TargetMol Chemicals Inc. | ||
 |
2024-11-01 | LY-364947
396129-53-6
|
US $0.00-0.00 / g | 1g | 98% | 1000kgs | Wuhan Nutra Biotechnology Co.,Ltd | |
 |
2019-09-06 | LY-364947
396129-53-6
|
US $1.00 / KG | 1KG | 98% | 20kg | Career Henan Chemical Co |
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