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Cat. No. M1772
PKI-587 Structure


Size Price Availability Quantity
5mg USD 100  USD100 In stock
10mg USD 180  USD180 In stock
50mg USD 520  USD520 In stock
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Quality Control & Documentation
Biological Activity

PKI-587 (PF-05212384) is a highly potent dual PI3K/mTOR kinase inhibitor.PKI-587 (PF-05212384)potently inhibited class I PI3Ks (IC (50) vs. PI3K-α = 0.4 nmol/L), PI3K-α mutants, and mTOR.PKI-587 (PF-05212384) inhibited growth of 50 diverse human tumor cell lines at IC (50) values of less than 1nm.PKI-587 (PF-05212384) also inhibit 236 human protein kinases (IC50s >10 μM.Only wild type and mutant (V600E) B-Rafs were inhibited by PKI-587 at IC50 values of 10μM.

Customer Product Validations & Biological Datas
Source Br J Cancer (2014). Figure 1. PKI-587
Method MTT assay
Cell Lines HNSCC cell lines
Concentrations 10–5000 nm
Incubation Time -
Results All the human squamous cell lines were highly sensitive to PKI-587, with an IC50 value ⩽100 nm
Chemical Information
Molecular Weight 615.73
Formula C32H41N9O4
CAS Number 1197160-78-3
Solubility (25°C) DMSO 2 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Gedaly R, et al. J Surg Res. PKI-587 and sorafenib targeting PI3K/AKT/mTOR and Ras/Raf/MAPK pathways synergistically inhibit HCC cell proliferation.

[2] Mallon R, et al. Clin Cancer Res. Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor.

[3] Venkatesan AM, et al. J Med Chem. Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.

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Abmole Inhibitor Catalog

Keywords: PKI-587, PF-05212384 supplier, PI3K, inhibitors, activators

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