LOXO-292
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- CAS-Nr.
- 2152628-33-4
- Englisch Name:
- LOXO-292
- Synonyma:
- SELPERCATINIB;LOX-292;CPD2206;LOX0292;Orapani;LOXO-292;ARRY-192);Secatinib;Serpatinib;Selpercatinib API
- CBNumber:
- CB34805442
- Summenformel:
- C29H31N7O3
- Molgewicht:
- 525.6
- MOL-Datei:
- 2152628-33-4.mol
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LOXO-292 Eigenschaften
- Dichte
- 1.36±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- L?slichkeit
- DMSO:20.0(Max Conc. mg/mL);38.05(Max Conc. mM)
- Aggregatzustand
- A crystalline solid
- pka
- 14.00±0.29(Predicted)
- Farbe
- White to off-white
- InChIKey
- XIIOFHFUYBLOLW-UHFFFAOYSA-N
- SMILES
- C12=C(C#N)C=NN1C=C(OCC(O)(C)C)C=C2C1=CC=C(N2CC3CC(N3CC3=CC=C(OC)N=C3)C2)N=C1
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 |
| P261 |
Einatmen von Staub vermeiden. |
| P280 |
Schutzhandschuhe/Schutzkleidung/Augenschutz tragen. |
| P301+P312 |
BEI VERSCHLUCKEN: Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen. |
| P302+P352 |
BEI BERüHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckm??ig, 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 M?glichkeit entfernen. Weiter spülen. |
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LOXO-292 Chemische Eigenschaften,Einsatz,Produktion Methoden
Verwenden
Selpercatinib(LOXO-292) is a highly selective, potent RET inhibitor, an oral drug used to treat cancers in people whose tumours have been altered (mutated or fused) in specific genes (RET stands for "rearrangement during transfection").
Trademarks
Retevmo
Nebenwirkungen
LOXO-292(Selpercatinib) can cause serious side effects including liver toxicity, high blood pressure, heart rhythm changes due to prolongation of heart electrical activity (QT prolongation), bleeding, allergic reactions, impaired wound healing and harm to an unborn baby.
Synthese
The sulfonyl chloride starting material 329 was reacted with tert-butyl hydroxyurea (330) under basic conditions and subsequently treated with trifluoroacetic acid (TFA) to afford O-sulfonylhydroxylamine 332. O-sulfonylhydroxylamine 332, as a nitrogen source, reacted with pyridine 333 to afford N-aminopyridinium salt 334. N-aminopyridinium salt 334 was further reacted with 2-chloroacrylonitrile (335) to establish the pyrazolopyridine core 336. Removal of the methyl ether using dodecanethiol (337) in warm dimethylformamide under basic conditions afforded the phenolic compound 338. Phenol 338 was converted to the triflate (339). The triflate 339 was cross-coupled with the boronate ester 340 under Suzuki conditions to react specifically at the triflate position with retention of the bromide to afford 341. 341 was reacted with the epoxide 342 under palladium catalysis to establish the ether side chain. Finally, the azabicyclic addendum 344 was installed via an NMR aromatic substitution reaction to generate salacartinib in 86% yield.
LOXO-292 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
LOXO-292 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 220)Lieferanten
- CPD2206
- LOXO-292; LOXO292;LOXO 292
- LOXO-292,Selpercatinib
- Selpercatinib(LOXO-292)
- 6-?(2-?Hydroxy-?2-?methylpropoxy)?-?4-?[6-?[6-?[(6-?methoxy-?3-?pyridinyl)?methyl]?-?3,?6-?diazabicyclo[3.1.1]?hept-?3-?yl]?-?3-?pyridinyl]?pyrazolo[1,?5-?a]?pyridine-?3-?carbonitrile
- Pyrazolo[1,5-a]pyridine-3-carbonitrile, 6-(2-hydroxy-2-methylpropoxy)-4-[6-[6-[(6-methoxy-3-pyridinyl)methyl]-3,6-diazabicyclo[3.1.1]hept-3-yl]-3-pyridinyl]-
- LOXO-292 USP/EP/BP
- 6-(2-hydroxy-2-methylpropoxy)-4-[6-[6-[(6-methoxypyridin-3-yl)methyl]-3,6-diazabicyclo[3.1.1]heptan-3-yl]pyridin-3-yl]pyrazolo[1,5-a]pyridine-3-carbonitrile
- Inhibitor LOXO-292
- ARRY-192)
- LOX-292
- Selpercatinib (LOXO-292, ARRY-192)
- LOX0292
- Serpatinib
- SELPERCATINIB
- LOXO-292
- 13C,2H3]-Selpercatinib
- Diethyl N-[5-[N-[(3,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)
methyll-N-methylamino]-2-thenoyll-L-glutamate
- Orapani
- Selpatinib LOXO-292
- Selpercatinib API
- Selpercatinib, 10 mM in DMSO
- Secatinib
- 2152628-33-4
- GS
- API
- 2152628-33-4
