LY 2157299
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- CAS-Nr.
- 700874-72-2
- Englisch Name:
- LY 2157299
- Synonyma:
- CS-5;LY 2157299;GALUNISERTIB;Galunisertib D6;LY2157299, >=98%;LY 2157299 USP/EP/BP;LY-2157299;LY 2157299;LY2157299,Galunisertib;Galunisertib,LY2157299;LY-2157299;LY 2157299;GALUNISERTIB
- CBNumber:
- CB02526184
- Summenformel:
- C22H19N5O
- Molgewicht:
- 369.42
- MOL-Datei:
- 700874-72-2.mol
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LY 2157299 Eigenschaften
- Schmelzpunkt:
- 241-242°C
- Siedepunkt:
- 619.0±55.0 °C(Predicted)
- Dichte
- 1.40
- Flammpunkt:
- 328.162℃
- storage temp.
- -20°C
- Löslichkeit
- Soluble in DMSO (up to 25 mg/ml)
- Aggregatzustand
- solid
- pka
- 15.27±0.30(Predicted)
- Farbe
- White
- Stabilität:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
- CAS Datenbank
- 700874-72-2
Sicherheit
- Risiko- und Sicherheitserklärung
- Gefahreninformationscode (GHS)
| Kennzeichnung gefährlicher |
T |
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| R-Sätze: |
25 |
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| S-Sätze: |
45 |
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| HS Code |
29334900 |
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| Bildanzeige (GHS) |
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| Alarmwort |
Warnung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| 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 |
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| Sicherheit |
| P280 |
Schutzhandschuhe/Schutzkleidung/Augenschutz tragen. |
| P302+P352 |
BEI BERÜHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckmäßig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen. |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen. |
| P332+P313 |
Bei Hautreizung: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen. |
| P337+P313 |
Bei anhaltender Augenreizung: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen. |
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LY 2157299 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Galunisertib (LY2157299 monohydrate) is a small-molecule inhibitor of TGFβR1 that binds antagonistically to TGFR1 to prevent the intracellular phosphorylation of SMAD2 and SMAD3.Phase I studies have demonstrated that galunisertib had an acceptable tolerability and safety profile in patients with advanced solid tumors.Recently the preclinical studies from Tran et al. demonstrated that galunisertib combined with anti-GD2 antibody Dinutuximab augmented the anti-tumor cytotoxicity of activated NK(aNK) cells which were activated ex vivo with K562.mbIL21 artificial antigen presenting cells.Galunisertib suppressed SMAD2 phosphorylation and restored the expression of DNAX Accessory Molecule-1,NKp30, NKG2D and TNF-related apoptosis-inducing ligand death ligand expression on aNK cells and also significantly enhanced the release of perforin and granzyme A from aNK cells and the direct cytotoxicity and ADCC of aNK cells against neuroblastoma cells in vitro.The combination of galunisertib, aNK cells plus dinutuximab reduced tumor growth and increased survival of mice xenografted with two neuroblastoma cell lines or a patient derived xenograft.In another study,galunisertib was shown to preserve the cytotoxic function of ex vivo expanded, highly activated NK cells and significantly improved eradication of liver metastases of colon cancer in mice treated with adoptive NK cells compared with mice receiving NK cells or TGF beta inhibition alone. Overall these studies demonstrate that the therapeutic efficacy of adoptive NK cell therapy clinically will be markedly enhanced by complementary approaches targeting TGF-beta signaling in vivo.
Verwenden
LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1 kinase (IC50 = 56 nM). It has been used to study the role of TGF-β signaling in chemotherapy-induced expansion of cancer stem-like cells in triple negative breast cancer cell lines and xenografts. LY2157299 has also been shown to inhibit the migration and tumor growth of hepatocellular carcinoma cell lines by disrupting Smad-2 phosphorylation.[Cayman Chemical]
LY 2157299 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
LY 2157299 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.
Global( 198)Lieferanten
700874-72-2()Verwandte Suche:
- LY 2157299
- 4-[5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide
- 6-QuinolinecarboxaMide, 4-[5,6-dihydro-2-(6-Methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-
- 4-[2-(6-Methyl-2-pyridinyl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxaMideorLY2157299
- GALUNISERTIB
- Galunisertib,LY2157299
- 4-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide
- 4-[5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide LY 2157299
- LY2157299,Galunisertib
- LY2157299, >=98%
- LY-2157299;LY 2157299;GALUNISERTIB
- Galunisertib, 98%, a potent TGF-β receptor I (TβRI) inhibitor
- CS-5
- 2-(6-methylpyridin-2-yl)-3-(6-aminocarbonylquinolin-4-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole
- LY-2157299;LY 2157299
- 4-[2-(6-Methylpyridin-2-yl)-4H,5H,6H-pyrrolo[1,2-b]pyrazol-3-yl]quinoline-6-carboxamide
- LY 2157299 USP/EP/BP
- Galunisertib D6
- 700874-72-2
- Inhibitors
- Smad
- TGF-beta
