Onalespib
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- CAS-Nr.
- 912999-49-6
- Englisch Name:
- Onalespib
- Synonyma:
- AT-13387;CS-1866;Onalespib;ATI-13387;ATI13387X;AT13387, >=98%;Onalespib Lactate;AT13387(Onalespib);ONALESPIB;ATI-13387;Onalespib (AT13387)
- CBNumber:
- CB32566420
- Summenformel:
- C24H31N3O3
- Molgewicht:
- 409.52
- MOL-Datei:
- 912999-49-6.mol
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Onalespib Eigenschaften
- Siedepunkt:
- 605.7±55.0 °C(Predicted)
- Dichte
- 1.237
- storage temp.
- Store at -20°C
- L?slichkeit
- insoluble in H2O; ≥13.25 mg/mL in DMSO; ≥47.7 mg/mL in EtOH with ultrasonic
- Aggregatzustand
- solid
- pka
- 8.50±0.48(Predicted)
- Farbe
- White to off-white
- InChI
- InChI=1S/C24H31N3O3/c1-16(2)20-11-21(23(29)12-22(20)28)24(30)27-14-18-5-4-17(10-19(18)15-27)13-26-8-6-25(3)7-9-26/h4-5,10-12,16,28-29H,6-9,13-15H2,1-3H3
- InChIKey
- IFRGXKKQHBVPCQ-UHFFFAOYSA-N
- SMILES
- C(N1CC2=C(C1)C=CC(CN1CCN(C)CC1)=C2)(C1=CC(C(C)C)=C(O)C=C1O)=O
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 |
| H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
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P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
Verursacht schwere Augenreizung. |
Schwere Augenreizung |
Kategorie 2 |
Warnung |
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P264, P280, P305+P351+P338,P337+P313P |
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| Sicherheit |
| P261 |
Einatmen von Staub vermeiden. |
| 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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Onalespib Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Onalespib, also known as AT13387, is a selective inhibitor of Hsp90 (IC50 = 18 nM). It induces the degradation of specific Hsp90 client proteins, including mutant EGFR, for up to seven days in tumor cell lines in vitro and up to three days in vivo. Onalespib is retained in tumor xenografts and is efficacious in a range of xenograft models. It differs from other HSP90 inhibitors in its longer duration of target inhibition and its favorable toxicity profile in phase I studies in patients with refractory solid tumors.
Mode of action
Onalespib selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins and has been used as a biomarker of HSP90 inhibition.
Einzelnachweise
Efficacy of Onalespib, a Long-Acting Second-Generation HSP90 Inhibitor, as a Single Agent and in Combination with Temozolomide against Malignant Gliomashttps://pubchem.ncbi.nlm.nih.gov/compound/Onalespib
Onalespib Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Onalespib Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 142)Lieferanten
- (2,4-dihydroxy-5-isopropylphenyl)(5-((4-Methylpiperazin-1-yl)Methyl)isoindolin-2-yl)Methanone
- 4-({5-[(4-Methylpiperazin-1-yl)Methyl]-2,3-dihydro-1H-isoindol-2-yl}carbonyl)-6-(propan-2-yl)benzene-1,3-diol
- [1,3-Dihydro-5-[(4-methyl-1-piperazinyl)methyl]-2H-isoindol-2-yl][2,4-dihydroxy-5-(1-methylethyl)phenyl]methanone
- Onalespib
- Onalespib (AT13387)
- [1,3-Dihydro-5-[(4-methyl-1-piperazinyl)methyl]-2H-isoindol-2-yl][2,4-dihydroxy-5-(1-methylethyl)phenyl]methanone AT13387
- AT13387, >=98%
- Onalespib Lactate
- (2,4-dihydroxy-5-isopropylphenyl)(5-((4-Methylpiperazin-1-yl)Methyl)isoindolin-2-yl)Methanone USP/EP/BP
- Methanone, [1,3-dihydro-5-[(4-methyl-1-piperazinyl)methyl]-2H-isoindol-2-yl][2,4-dihydroxy-5-(1-methylethyl)phenyl]-
- ONALESPIB;ATI-13387
- ATI-13387
- (2,4-dihydroxy-5-propan-2-ylphenyl)-[5-[(4-methylpiperazin-1-yl)methyl]-1,3-dihydroisoindol-2-yl]methanone
- AT13387(Onalespib)
- CS-1866
- ATI13387X
- Onalespib AT-13387 AT13387
- Onalespib, 10 mM in DMSO
- Onalespib (AT13387) ，S1163
- AT-13387
- 912999-49-6
- 12999-49-6
- Inhibitor
- Inhibitors
