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Sapanisertib

Chemical Structure : Sapanisertib

CAS No.: 1224844-38-5

Sapanisertib (INK-128, MLN0128, TAK-228, CB-228)

Catalog No.: PC-43497Not For Human Use, Lab Use Only.

Sapanisertib (INK-128, MLN0128, TAK-228) is a potent, ATP-competitive, orally active dual mTORC1/2 inhibitor with Ki of 1.4 nM in cell-free assays, >200-fold selectivity over calss I PI3K isoforms.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Sapanisertib (INK-128, MLN0128, TAK-228) is a potent, ATP-competitive, orally active dual mTORC1/2 inhibitor with Ki of 1.4 nM in cell-free assays, >200-fold selectivity over calss I PI3K isoforms.
Sapanisertib (INK-128, MLN0128) inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inhibits AKT phosphorylation at Ser473, the downstream substrate of TORC2.
Sapanisertib (INK-128, MLN0128) also shows potent inhibition effects on cell lines resistant to rapamycin and pan-PI3K inhibitors.
Sapanisertib (INK-128, MLN0128) shows tumor growth inhibition efficacy in multiplexenograft models.

Physicochemical Properties

M.Wt 309.33
Formula C15H15N7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 3-(2-amino-5-benzoxazolyl)-1-(1-methylethyl)-

References

1. Hsieh AC, et al. Nature. 2012 Feb 22;485(7396):55-61.

2. Gökmen-Polar Y, et al. Breast Cancer Res Treat.

3. Maiso P, et al. Blood. 2011 Dec 22;118(26):6860-70.

4. Janes MR, et al. Leukemia. 2013 Mar;27(3):586-94.

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