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Signal Inhibitors and Activators
PKI-587
$633.6/ 5mg1 PHYSICAL AND CHEMICAL PROPERTIES
QuantityTotal: $634
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Product Information
Kinase Inhibitor Name PKI-587
FormulaC32H41N9O4
SolubilityDMSO ≥9 mg/mL Water <1 mg/mL Ethanol ≥1 mg/mL
Stability:
2 years -20℃ Powder
1 week -4℃ in DMSO
1 month -80℃ in DMSO
Stability:
2 years -20℃ Powder
1 week -4℃ in DMSO
1 month -80℃ in DMSO
CAS No.1197160-78-3
Molecular Structure2 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]
3 References:
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.
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]
3 References:
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.
M.W.615.73
Price633.5999999999999$
Research AreaStem Cells Cancer Cardiovascular Cell Biology Epigenetics & Nuclear Signaling Developmental Biologys Immunology Drug Discovery Products Metabolism Neuroscience Signal Transduction
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