LOXO-101
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- CAS-Nr.
- 1223403-58-4
- Englisch Name:
- LOXO-101
- Synonyma:
- Larotrectinib;(3S)-N-[5-[(2R)-2-(2,5-Difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-1-pyrrolidinecarboxamide;Larotrec;(R)-N-(5-((S)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide;CS-2322;LOXO 10;ARRY 470;LOXO-101;ROM for Nepal;LOXO101;LOXO 101
- CBNumber:
- CB53121981
- Summenformel:
- C21H22F2N6O2
- Molgewicht:
- 428.44
- MOL-Datei:
- 1223403-58-4.mol
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LOXO-101 Eigenschaften
- Dichte
- 1.55±0.1 g/cm3(Predicted)
- storage temp.
- RT
- L?slichkeit
- Soluble in DMSO (up to 5 mg/ml).
- Aggregatzustand
- solid
- pka
- 8.41±0.40(Predicted)
- Farbe
- Yellow
- Stabilit?t:
- Stable for 1 year 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
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| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H302 |
Gesundheitssch?dlich bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 4 |
Warnung |
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P264, P270, P301+P312, P330, P501 |
| H317 |
Kann allergische Hautreaktionen verursachen. |
Sensibilisierung der Haut |
Kategorie 1A |
Warnung |
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P261, P272, P280, P302+P352,P333+P313, P321, P363, P501 |
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| Sicherheit |
| P280 |
Schutzhandschuhe/Schutzkleidung/Augenschutz tragen. |
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LOXO-101 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
LOXO-101 is an inhibitor of the tropomyosin-related kinases TrkA, TrkB, and TrkC (IC
50s = 2-20 nM). It is selective for TrkA, -B, and -C over a panel of 226 kinases at 1 μM. LOXO-101 inhibits the growth of CUTO-3.29, KM12, and MO-91 patient-derived cancer cell lines (IC
50s = <100, <10, and <10 nM, respectively).
In vivo, LOXO-101 (60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model.
Beschreibung
Larotrectinib, also known as LOXO-101 and ARRY-470, is a small molecule that was designed to block the ATP-binding site of the TRKA, TRKB, and TRKC, serving as a highly specific and potent inhibitor of all of the three tropomyosin kinase receptors.
Verwenden
Larotrectinib is a TRK Inhibitor (Tyrosine kinase inhibitor).
Trademarks
Vitrakvi
Clinical Use
The US Food and Drug Administration (FDA) granted accelerated approval to larotrectinib (Vitrakvi) on November 26th, 2018, as a treatment for adult and pediatric patients with solid tumors that have NTRK gene fusions without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have no satisfactory alternative treatments or that have progressed following treatment on. In the approval statement by FDA, a complete response rate of 22% and partial response rate of 53% were cited.
LOXO-101 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
LOXO-101 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 244)Lieferanten
- LOXO-101
- ARRY 470
- (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
- LOXO-101 (ARRY-470)
- CS-2322
- LOXO101;LOXO 101
- LOXO-101 Larotrectinib
- LOXO-101 (ARRY-470,Larotrectinib)
- LOXO-101,LAROTRECTINIB,ARRY-470
- Larotrectinib base
- 1-Pyrrolidinecarboxamide, N-[5-[(2R)-2-(2,5-difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-, (3S)-
- LOXO101（free base）
- ROM for Nepal
- LOXO 10
- (3S)-N-{5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl}-3-hydroxypyrrolidine-1-carboxamide
- Larotrec
- LarotrectinibFor
- Larotrectinib, 10 mM in DMSO
- (3S)-N-[5-[(2R)-2-(2,5-Difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-1-pyrrolidinecarboxamide
- (R)-N-(5-((S)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
- Larotrectinib
- 1223403-58-4
- 1223403-66-1
- C21H22F2N6O2
- API
- APIs
