A-83-01
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- CAS-Nr.
- 909910-43-6
- Englisch Name:
- A-83-01
- Synonyma:
- CS-578;A 83-01, >=98%;A 83-01;A83-01;A-83-01AB142092);ALK5 Inhibitor IV;TGF inhibitor A-83-01;A 83-01 (DMSO solution;TGF-β RI Kinase Inhibitor IV;A83-01; A-83-01;A8301;A-8301;A 8301;TGF-β RI Kinase Inhibitor IV - CAS 909910-43-6 - Calbiochem
- CBNumber:
- CB9972670
- Summenformel:
- C25H19N5S
- Molgewicht:
- 421.52
- MOL-Datei:
- 909910-43-6.mol
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A-83-01 Eigenschaften
- Schmelzpunkt:
- 111℃
- Siedepunkt:
- 590.0±60.0 °C(Predicted)
- Dichte
- 1.27±0.1 g/cm3(Predicted)
- storage temp.
- -20°C
- L?slichkeit
- DMSO: soluble5mg/mL, clear (warmed)
- pka
- 8.77±0.70(Predicted)
- Aggregatzustand
- powder
- Farbe
- white to beige
- Stabilit?t:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
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| Alarmwort |
Warnung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H302 |
Gesundheitssch?dlich bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 4 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P270, P301+P312, P330, P501 |
| H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
Verursacht schwere Augenreizung. |
Schwere Augenreizung |
Kategorie 2 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P305+P351+P338,P337+P313P |
| H335 |
Kann die Atemwege reizen. |
Spezifische Zielorgan-Toxizit?t (einmalige Exposition) |
Kategorie 3 (Atemwegsreizung) |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
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| Sicherheit |
| P280 |
Schutzhandschuhe/Schutzkleidung/Augenschutz tragen. |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen. |
| P337+P313 |
Bei anhaltender Augenreizung: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen. |
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A-83-01 Chemische Eigenschaften,Einsatz,Produktion Methoden
Verwenden
A 83-01 is a selective inhibitor of TGF-β type I receptor. A 83-01 treatment increases tumor permeability.
Biologische Aktivit?t
Selective inhibitor of TGF- β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC 50 values are 12, 45 and 7.5 nM respectively). Blocks phosphorylation of Smad2 and inhibits TGF- β -induced epithelial-to-mesenchymal transition. Only weakly inhibits ALK-1, -2, -3, -6 and MAPK activity. More potent than SB 431542 (4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol -2-yl]benzamide). Inhibits differentiation of rat induced pluripotent stem cells (riPSCs) and increases clonal expansion efficiency. Helps maintain homogeneity and long-term in vitro self-renewal of human iPSCs.
Enzyminhibitor
This TGFb inhibitor (FW = 421.52 g/mol; CAS 909910-43-6; Solubility: 50 mM in DMSO), named 3-(6-methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide, selectively targets TGF-β type I receptor ALK5 kinase (IC50 = 12 nM), Type I Activin/Nodal receptor ALK4 (IC50 = 45 nM), and type I nodal receptor ALK7 (IC50 = 7.5 nM), blocking the phosphorylation of Smad2 and inhibiting TGF-β-induced epithelial-to-mesenchymal transitions. TGF-β signaling inhibitors represent a useful strategy for treating patients with tumor growth and metastasis in advanced cancer. A-83-01 only weakly inhibits ALK-1, ALK-2, ALK-3, ALK-6 and MAPK. It also has little or no effect on bone morphogenetic protein type I receptors, p38 mitogen-activated protein kinase, or extracellular regulated kinase. A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Its use also instrumental in demonstrating that attachment to Laminin-111 facilitates TGF-β-induced expression of matrix metalloproteinase-2 in synovial fibroblasts.
A-83-01 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
A-83-01 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 121)Lieferanten
- A 83-01;A83-01
- TGF inhibitor A-83-01
- 3-(6-methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide
- TGF-β RI Kinase Inhibitor IV
- A 83-01, >=98%
- 3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide
- A-83-01AB142092)
- ALK5 Inhibitor IV
- 1H-Pyrazole-1-carbothioamide,3-(6-methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-
- 3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide
- A83-01; A-83-01;A8301;A-8301;A 8301
- TGF-β RI Kinase Inhibitor IV - CAS 909910-43-6 - Calbiochem
- CS-578
- A 83-01 (DMSO solution
- 3-(6-Methyl-2-pyridyl)-N-phenyl-4-(4-quinolinyl)pyrazole-1-carbothioamide
- 909910-43-6
- C25H19N5S
- Inhibitors
- TGF-beta/Smad
- Protein Kinase
