A66
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- CAS-Nr.
- 1166227-08-2
- Englisch Name:
- A66
- Synonyma:
- CS-435;A 66;A-66;A66 USP/EP/BP;A66 PI3K inhibitor A-66;A66, 98%, a potent and specific p110α inhibitor;Phosphoinositide 3-kinase,inhibit,PI3K,A66,Inhibitor,A-66,A 66;(2S)-N1-[2-(tert-Butyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-1,2-pyrrolidinedicarboxamide;(S)-N1-(2-(tert-Butyl)-4'-methyl-[4,5'-bithiazol]-2'-yl)pyrrolidine-1,2-dicarboxamide;(2S)-N1-(5-(2-tert-butylthiazol-4-yl)-4-methylthiazol-2-yl)pyrrolidine-1,2-dicarboxamide;(2S)-N1-[2-(1,1-Dimethylethyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-1,2-pyrrolidinedicarboxamide
- CBNumber:
- CB42553771
- Summenformel:
- C17H23N5O2S2
- Molgewicht:
- 393.53
- MOL-Datei:
- 1166227-08-2.mol
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A66 Eigenschaften
- Dichte
- 1.354
- storage temp.
- Sealed in dry,Store in freezer, under -20°C
- L?slichkeit
- insoluble in H2O; ≥19.7 mg/mL in DMSO; ≥2.63 mg/mL in EtOH with gentle warming
- Aggregatzustand
- solid
- pka
- 6.27±0.70(Predicted)
- Farbe
- Off-white to light yellow
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 |
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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. |
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A66 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
A-66 is a potent, selective inhibitor of the PI3K isoform p110α (IC
50 = 32 nM in a cell-free assay). It displays over 100-fold selectivity for p110α over other isoforms. A-66 is effective
in vivo, suppressing the growth of SK-OV-3 tumor xenografts in mice. It also impairs all measures of
in vivo insulin action in mice. A-66 partially suppresses B cell receptor-dependent Akt activation and proliferation.
Enzyminhibitor
This potent and highly selective p110α inhibitor (FW = 393.53; CAS 1166227-08-2; Solubility: 79 mg/mL DMSO, 1 mg/mL H2O), also known as (2S)-N1-(5-(2-tert-butylthiazol-4-yl)-4-methylthiazol-2-yl)pyrrolidine-1, 2-dicarboxamide, has a IC50 value of 32 nM for the wild-type phosphoinositide-3 kinase p110 α as well as oncogenic forms of p110α such as p110α E545K (IC50 = 43 nM) and p110α H1047R (IC50 = 43 nM). A66 inhibition also demonstrated that cancer-specific mutations in the iSH2 (inter-SH2) and nSH2 (N-terminal SH2) domains of p85α, the regulatory subunit of phosphatidylinositide 3-kinase (PI3K), show gain of function, inducing oncogenic cellular transformation, stimulating cellular proliferation, and enhancing PI3K signaling.
A66 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
A66 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 113)Lieferanten
- (2S)-N1-[2-(tert-Butyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-1,2-pyrrolidinedicarboxamide
- (2S)-N1-(5-(2-tert-butylthiazol-4-yl)-4-methylthiazol-2-yl)pyrrolidine-1,2-dicarboxamide
- (2S)-N1-[2-(tert-Butyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-1,2-pyrrolidinedicarboxamide A 66
- CS-435
- A66, 98%, a potent and specific p110α inhibitor
- (2S)-N1-[2-(1,1-Dimethylethyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-1,2-pyrrolidinedicarboxamide
- A 66;A-66
- 1,2-Pyrrolidinedicarboxamide, N1-[2-(1,1-dimethylethyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-, (2S)-
- A66 USP/EP/BP
- A66 PI3K inhibitor A-66
- Phosphoinositide 3-kinase,inhibit,PI3K,A66,Inhibitor,A-66,A 66
- (S)-N1-(2-(tert-Butyl)-4'-methyl-[4,5'-bithiazol]-2'-yl)pyrrolidine-1,2-dicarboxamide
- 1166227-08-2
- C17H23N5O2S2
- Inhibitors
- Akt
- mTOR
- PI3K
- PI3K/Akt/mTOR
