PF 05212384

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Cat.No. 4823 - PF 05212384 | C32H41N9O4 | CAS No. 1197160-78-3
Description: Potent and selective dual PI 3-K/mTOR inhibitor
Alternative Names: PKI-587, Gedatolisib
Chemical Name: N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)phenyl]urea
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity

Potent and selective dual inhibitor of PI 3-kinase/mTOR (IC50 values are 0.4, 1.6 and 5.4 nM for PI 3-Kα, mTOR and PI 3-Kγ respectively). Exhibits selectivity over 234 other protein kinases (IC50 >10 μM). Potently inhibits tumor cell growth in 37 different tumor cell lines (IC50 < 100 nM). Also exhibits antitumor activity in MDA-361, HCT-116, H1975 and U87MG xenograft models.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 615.73
Formula C32H41N9O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1197160-78-3
PubChem ID 44516953
InChI Key DWZAEMINVBZMHQ-UHFFFAOYSA-N
Smiles O=C(NC5=CC=C(C(N6CCC(N(C)C)CC6)=O)C=C5)NC(C=C4)=CC=C4C1=NC(N2CCOCC2)=NC(N3CCOCC3)=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 3.08 5 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 615.73. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.05 mM 32.48 mL 162.41 mL 324.82 mL
0.25 mM 6.5 mL 32.48 mL 64.96 mL
0.5 mM 3.25 mL 16.24 mL 32.48 mL
2.5 mM 0.65 mL 3.25 mL 6.5 mL

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References

References are publications that support the biological activity of the product.

Venkatesan et al (2010) 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. J.Med.Chem. 53 2636 PMID: 20166697

Mallon et al (2011) Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clin.Cancer Res. 17 3193 PMID: 21325073


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Keywords: PF 05212384, PF 05212384 supplier, PF05212384, antitumor, antitumour, PI3-K, phosphoinositide, 3-kinases, mTOR, mammalian, target, of, rapamycin, inhibitors, inhibits, PKI587, Pfizer, PKI-587, Gedatolisib, PI, 3-Kinase, 4823, Tocris Bioscience

Citations for PF 05212384

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