694433-59-5,MFCD20926329
Catalog No.:AA00FBY8

694433-59-5 | SB-505124

Pack Size
Purity
Availability
Price(USD)
Quantity
  
1mg
≥98%
in stock  
$53.00   $37.00
- +
5mg
98%
in stock  
$100.00   $70.00
- +
10mg
98%
in stock  
$156.00   $109.00
- +
25mg
98%
in stock  
$237.00   $166.00
- +
50mg
98%
in stock  
$408.00   $286.00
- +
100mg
98%
in stock  
$585.00   $409.00
- +
  • Technical Information
  • Properties
  • Literature
  • Request for Quotation
  • Download SDS
Technical Information
Catalog Number:
AA00FBY8
Chemical Name:
SB-505124
CAS Number:
694433-59-5
Molecular Formula:
C20H21N3O2
Molecular Weight:
335.3996
MDL Number:
MFCD20926329
SMILES:
Cc1cccc(n1)c1[nH]c(nc1c1ccc2c(c1)OCO2)C(C)(C)C
Properties
Computed Properties
 
Complexity:
466  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
0  
Defined Bond Stereocenter Count:
0  
Formal Charge:
0  
Heavy Atom Count:
25  
Hydrogen Bond Acceptor Count:
4  
Hydrogen Bond Donor Count:
1  
Isotope Atom Count:
0  
Rotatable Bond Count:
3  
Undefined Atom Stereocenter Count:
0  
Undefined Bond Stereocenter Count:
0  
XLogP3:
4.3  

Literature

Title: Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent.

Journal: Journal of medicinal chemistry 20140522

Title: A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.

Journal: The Biochemical journal 20130415

Title: NODAL and SHH dose-dependent double inhibition promotes an HPE-like phenotype in chick embryos.

Journal: Disease models & mechanisms 20130301

Title: Endothelial cell transforming growth factor-β receptor activation causes tacrolimus-induced renal arteriolar hyalinosis.

Journal: Kidney international 20121001

Title: Cdk4/6 inhibition induces epithelial-mesenchymal transition and enhances invasiveness in pancreatic cancer cells.

Journal: Molecular cancer therapeutics 20121001

Title: Yin-Yang1 is required for epithelial-to-mesenchymal transition and regulation of Nodal signaling during mammalian gastrulation.

Journal: Developmental biology 20120815

Title: Transforming growth factor-β2 induces synthesis and secretion of endothelin-1 in human trabecular meshwork cells.

Journal: Investigative ophthalmology & visual science 20120807

Title: Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.

Journal: Nature biotechnology 20111101

Title: Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.

Journal: European journal of medicinal chemistry 20110901

Title: Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.

Journal: Bioorganic & medicinal chemistry 20110415

Title: Smad signaling determines chondrogenic differentiation of bone-marrow-derived mesenchymal stem cells: inhibition of Smad1/5/8P prevents terminal differentiation and calcification.

Journal: Tissue engineering. Part A 20110401

Title: Synthesis and biological evaluation of 2-pyridyl-substituted pyrazoles and imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20100715

Title: Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.

Journal: Bioorganic & medicinal chemistry 20100615

Title: Hydrogen sulfide attenuates epithelial-mesenchymal transition of human alveolar epithelial cells.

Journal: Pharmacological research 20100401

Title: Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by activin receptor-like kinase 5 inhibitor.

Journal: Molecular vision 20100101

Title: Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles as inhibitors of transforming growth factor beta type 1 receptor (ALK5).

Journal: Bioorganic & medicinal chemistry letters 20090815

Title: TGF-beta1 induced MMP-9 expression in HNSCC cell lines via Smad/MLCK pathway.

Journal: Biochemical and biophysical research communications 20080711

Title: The essential role of fibroblasts in esophageal squamous cell carcinoma-induced angiogenesis.

Journal: Gastroenterology 20080601

Title: TGF-beta signaling promotes survival and repair in rat alveolar epithelial type 2 cells during recovery after hyperoxic injury.

Journal: American journal of physiology. Lung cellular and molecular physiology 20080401

Title: Synthesis and biological evaluation of 5-(pyridin-2-yl)thiazoles as transforming growth factor-beta type1 receptor kinase inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20080315

Title: The role of maternal Activin-like signals in zebrafish embryos.

Journal: Developmental biology 20070915

Title: Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.

Journal: Journal of medicinal chemistry 20070628

Title: Time-dependent patterning of the mesoderm and endoderm by Nodal signals in zebrafish.

Journal: BMC developmental biology 20070101

Title: SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7.

Journal: Molecular pharmacology 20040301

Title: DaCosta Byfield S, et al. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2004 Mar;65(3):744-52.

Title: Sutariya V, et al. Thermoreversible gel for delivery of receptor-like kinase 5 inhibitor SB-505124 for glaucoma filtration surgery. Pharm Dev Technol. 2013 Jul-Aug;18(4):957-62.

Title: Sapitro J, et al. Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by receptor-like kinase 5 inhibitor. Mol Vis. 2010 Sep 16;16:1880-92.

Title: Marini KD, et al. Inhibition of activin signaling in lung adenocarcinoma increases the therapeutic index of platinum chemotherapy. Sci Transl Med. 2018 Jul 25;10(451). pii: eaat3504.

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SDS
Tags:694433-59-5 Molecular Formula|694433-59-5 MDL|694433-59-5 SMILES|694433-59-5 SB-505124
Catalog No.: AA00FBY8
694433-59-5,MFCD20926329
694433-59-5 | SB-505124
Pack Size: 1mg
Purity: ≥98%
in stock
$53.00 $37.00
Pack Size: 5mg
Purity: 98%
in stock
$100.00 $70.00
Pack Size: 10mg
Purity: 98%
in stock
$156.00 $109.00
Pack Size: 25mg
Purity: 98%
in stock
$237.00 $166.00
Pack Size: 50mg
Purity: 98%
in stock
$408.00 $286.00
Pack Size: 100mg
Purity: 98%
in stock
$585.00 $409.00
Quantity
- +
Add to Card
Order Now
bulk Quotation Request
Technical Information
Catalog Number: AA00FBY8
Chemical Name: SB-505124
CAS Number: 694433-59-5
Molecular Formula: C20H21N3O2
Molecular Weight: 335.3996
MDL Number: MFCD20926329
SMILES: Cc1cccc(n1)c1[nH]c(nc1c1ccc2c(c1)OCO2)C(C)(C)C
Properties
Complexity: 466  
Covalently-Bonded Unit Count: 1  
Defined Atom Stereocenter Count: 0  
Defined Bond Stereocenter Count: 0  
Formal Charge: 0  
Heavy Atom Count: 25  
Hydrogen Bond Acceptor Count: 4  
Hydrogen Bond Donor Count: 1  
Isotope Atom Count: 0  
Rotatable Bond Count: 3  
Undefined Atom Stereocenter Count: 0  
Undefined Bond Stereocenter Count: 0  
XLogP3: 4.3  
Literature fold

Title: Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent.

Journal: Journal of medicinal chemistry20140522

Title: A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.

Journal: The Biochemical journal20130415

Title: NODAL and SHH dose-dependent double inhibition promotes an HPE-like phenotype in chick embryos.

Journal: Disease models & mechanisms20130301

Title: Endothelial cell transforming growth factor-β receptor activation causes tacrolimus-induced renal arteriolar hyalinosis.

Journal: Kidney international20121001

Title: Cdk4/6 inhibition induces epithelial-mesenchymal transition and enhances invasiveness in pancreatic cancer cells.

Journal: Molecular cancer therapeutics20121001

Title: Yin-Yang1 is required for epithelial-to-mesenchymal transition and regulation of Nodal signaling during mammalian gastrulation.

Journal: Developmental biology20120815

Title: Transforming growth factor-β2 induces synthesis and secretion of endothelin-1 in human trabecular meshwork cells.

Journal: Investigative ophthalmology & visual science20120807

Title: Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.

Journal: Nature biotechnology20111101

Title: Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.

Journal: European journal of medicinal chemistry20110901

Title: Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.

Journal: Bioorganic & medicinal chemistry20110415

Title: Smad signaling determines chondrogenic differentiation of bone-marrow-derived mesenchymal stem cells: inhibition of Smad1/5/8P prevents terminal differentiation and calcification.

Journal: Tissue engineering. Part A20110401

Title: Synthesis and biological evaluation of 2-pyridyl-substituted pyrazoles and imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.

Journal: Bioorganic & medicinal chemistry letters20100715

Title: Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.

Journal: Bioorganic & medicinal chemistry20100615

Title: Hydrogen sulfide attenuates epithelial-mesenchymal transition of human alveolar epithelial cells.

Journal: Pharmacological research20100401

Title: Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by activin receptor-like kinase 5 inhibitor.

Journal: Molecular vision20100101

Title: Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles as inhibitors of transforming growth factor beta type 1 receptor (ALK5).

Journal: Bioorganic & medicinal chemistry letters20090815

Title: TGF-beta1 induced MMP-9 expression in HNSCC cell lines via Smad/MLCK pathway.

Journal: Biochemical and biophysical research communications20080711

Title: The essential role of fibroblasts in esophageal squamous cell carcinoma-induced angiogenesis.

Journal: Gastroenterology20080601

Title: TGF-beta signaling promotes survival and repair in rat alveolar epithelial type 2 cells during recovery after hyperoxic injury.

Journal: American journal of physiology. Lung cellular and molecular physiology20080401

Title: Synthesis and biological evaluation of 5-(pyridin-2-yl)thiazoles as transforming growth factor-beta type1 receptor kinase inhibitors.

Journal: Bioorganic & medicinal chemistry letters20080315

Title: The role of maternal Activin-like signals in zebrafish embryos.

Journal: Developmental biology20070915

Title: Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.

Journal: Journal of medicinal chemistry20070628

Title: Time-dependent patterning of the mesoderm and endoderm by Nodal signals in zebrafish.

Journal: BMC developmental biology20070101

Title: SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7.

Journal: Molecular pharmacology20040301

Title: DaCosta Byfield S, et al. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2004 Mar;65(3):744-52.

Title: Sutariya V, et al. Thermoreversible gel for delivery of receptor-like kinase 5 inhibitor SB-505124 for glaucoma filtration surgery. Pharm Dev Technol. 2013 Jul-Aug;18(4):957-62.

Title: Sapitro J, et al. Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by receptor-like kinase 5 inhibitor. Mol Vis. 2010 Sep 16;16:1880-92.

Title: Marini KD, et al. Inhibition of activin signaling in lung adenocarcinoma increases the therapeutic index of platinum chemotherapy. Sci Transl Med. 2018 Jul 25;10(451). pii: eaat3504.

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