533637 Sigma-AldrichPI 3-Kα Inhibitor XXIV, A66 - CAS 1166227-08-2 - Calbiochem
A66, CAS 1166227-08-2, is a potent, selective, reversible, ATP-competitive inhibitor of wild-type and oncogenic forms of PI 3-K isoform p110a (IC₅₀ = 32, 30, 43 nM for p110a, p110aE545K, p110H1047R).
More>> A66, CAS 1166227-08-2, is a potent, selective, reversible, ATP-competitive inhibitor of wild-type and oncogenic forms of PI 3-K isoform p110a (IC₅₀ = 32, 30, 43 nM for p110a, p110aE545K, p110H1047R). Less<<SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.
Synonyme: A-66, (S)-form
Empfohlene Produkte
Übersicht
| Replacement Information |
|---|
Key Spec Table
| CAS # | Empirical Formula |
|---|---|
| 1166227-08-2 | C₁₇H₂₃N₅O₂S₂ |
| Description | |
|---|---|
| Overview | A cell-permeable, bioavailable aminothiazole compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of both wild-type and oncogenic forms of PI 3-K isoform p110α (IC50 = 32, 30 and 43 nM for p110α, p110αE545K and p110H1047R, respectively). Does not affect the activity of p110β, p110δ & p110γ (IC50 = 12.5, 1.25, and 3.4 µM, respectively). Exhibits greater selectivity over other PI 3-Ks (IC50 = 5.0, 0.462, 5.0, 5.0, 5.0, 5.0, and 0.236 µM for PI 3-KC2α, PI 3-KC2β, PI 3-K class-III, mTOR, DNA-PK, PI 4-Kα and PI 4-Kβ, respectively) and 318 other protein kinases. Displays greater selectivity than PIK-75 (Cat. No. 528116) and reduces Akt and p70S6 kinase phosphorylation. Shown to retard the growth of SK-OV-3 and HCT-116 xenografted tumors in mice (75 mg/kg, i.p, q.d). Exhibits desirable pharmacokinetic properties (Tmax = 30 min; t1/2= 0.42 h; Cmax: 8.247 µM; and AUC0-inf = 6.8 µM/h; at 10 mg/kg). Also, reported to increase plasma insulin levels and enhance production of glucose from pyruvate in CD1 mice (10 mg/kg, i.p.). Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water. |
| Catalogue Number | 533637 |
| Brand Family | Calbiochem® |
| Synonyms | A-66, (S)-form |
| Product Information | |
|---|---|
| CAS number | 1166227-08-2 |
| Form | White solid |
| Hill Formula | C₁₇H₂₃N₅O₂S₂ |
| Chemical formula | C₁₇H₂₃N₅O₂S₂ |
| Reversible | Y |
| Quality Level | MQ100 |
| Applications |
|---|
| Biological Information | |
|---|---|
| Primary Target | wild-type and oncogenic forms of PI 3-K isoform p110α |
| Primary Target IC<sub>50</sub> | 32, 30 and 43 nM for p110&alpha |
| Purity | ≥98% by HPLC |
| Physicochemical Information | |
|---|---|
| Cell permeable | Y |
| Dimensions |
|---|
| Materials Information |
|---|
| Toxicological Information |
|---|
| Safety Information according to GHS |
|---|
| Safety Information |
|---|
| Product Usage Statements |
|---|
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Transport Information |
|---|
| Supplemental Information |
|---|
| Specifications |
|---|
| Global Trade Item Number | |
|---|---|
| Bestellnummer | GTIN |
| 533637 | 0 |
Documentation
PI 3-Kα Inhibitor XXIV, A66 - CAS 1166227-08-2 - Calbiochem SDB
| Titel |
|---|
Literatur
| Übersicht |
|---|
| Holand, K., et al. 2014. PLoS ONE. 9, e94132. Smith, G.C., et al. 2012. Biochem. J., 442, 161. Jamieson, S., et al. 2011. Biochem. J., 438, 53. Waardenberg, A.J., et al. 2011. J. Biol. Chem. 286, 30837. Sun, M., et al. 2010. Proc. Natl. Acad. Sci. USA. 35, 15547. |
| Datenblatt | ||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
|