1197160-78-3
1197160-78-3
Chemical Structure
Gedatolisib
Synonym(s): PKI-587; PF-05212384
- CAS No.: 1197160-78-3
- Formula:C32H41N9O4
- Molecular Weight:615.73
IUPAC Name: 1-(4-(4-(dimethylamino)piperidine-1-carbonyl)phenyl)-3-(4-(4,6-dimorpholino-1,3,5-triazin-2-yl)phenyl)urea
InChIKey: DWZAEMINVBZMHQ-UHFFFAOYSA-N
SMILES: CN(C1CCN(C(C2=CC=C(NC(NC3=CC=C(C4=NC(N5CCOCC5)=NC(N6CCOCC6)=N4)C=C3)=O)C=C2)=O)CC1)C
Biological Activity: Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively[1]. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2[2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Gedatolisib | 99.89% | Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2. | ||||||||||||||||||||
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Gedatolisib (Standard) | 97.70% | Gedatolisib (Standard) is the analytical standard of Gedatolisib. This product is intended for research and analytical applications. Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2. | ||||||||||||||||||||
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Gedatolisib-d6 | Gedatolisib-d6 (PKI-587-d6) is the deuterium labeled Gedatolisib (HY-10681). Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2. | |||||||||||||||||||||
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Gedatolisib-d8 | Gedatolisib-d8 (PKI-587-d8) is the deuterium labeled Gedatolisib (HY-10681). Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2. | |||||||||||||||||||||
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References
- [1]. Venkatesan AM, et al. 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. 2010, 53(6), 2636-2645. [Content Brief]
- [2]. Freitag H, et al. Inhibition of mTOR's Catalytic Site by PKI-587 Is a Promising Therapeutic Option for Gastroenteropancreatic Neuroendocrine Tumor Disease. Neuroendocrinology. 2017;105(1):90-104. [Content Brief]
