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PKI-587 Chemical Structure
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Biological Activity
PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM and <0.1 μM for PI3K-α and mTOR, respectively. Intravenous administration of PKI-587 exhibits excellent antitumor activity in vitro and in vivo in both subcutaneous and orthotopic xenograft tumor models. Phosphorylation of PI3K/mTOR effectors (e.g., Akt) effectively inhibited by PKI-587. And PKI-587 induced apoptosis in human tumor cell lines with elevated PI3K/mTOR signaling. In vivo, PKI-587suppressed tumor growth in breast (MDA-MB-361, BT474), colon (HCT116), lung (H1975), and glioma (U87MG) xenograft models. PKI-587 (25 mg/kg, single dose i.v.) suppressed Akt phosphorylation [at threonine(T)308 and serine(S)473] for up to 36 hours, with cleaved PARP (cPARP) evident up to 18 hours in MDA-MB-361 tumors. PKI-587 also caused regression in other tumor models, and efficacy was enhanced when given in combination with PD0325901 (MEK 1/2 inhibitor), irinotecan (topoisomerase I inhibitor), or HKI-272 (neratinib, HER2 inhibitor). [1][2]
Chemical Information
| Molecular Weight (WM): | 615.73 |
|---|---|
| Formula: | C32H41N9O4 |
| CAS No.: | 1197160-78-3 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥9mg/mL |
| Water <1mg/mL | |
| Ethanol ≥1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of PKI-587 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of PKI-587 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
Data independently produced by Dr. Zhang of Tianjin Medical University PKI-587 purchased from Selleck
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After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of PKI-587 for 3h,followed by 20-minute stimolation of 100ng/ml EGF. |
Data independently produced by Dr. Zhang of Tianjin Medical University
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