Torkinib (PP242) is a selective mTOR inhibitor with an IC50 of 8 nM in cell-free trials. Targeting the mTOR complex, mTOR is more than 10 times more selective than PI3Kδ or PI3Kα/β/γ, respectively. Torkinib (PP242) can induce mitochondrial autophagy and apoptosis.

 

Brand: BCM

 

Target: Apoptosis; Mitophagy; PI3K; mTOR; Autophagy

 

Signaling Pathways: Apoptosis; Autophagy; PI3K/Akt/mTOR signaling

 

In Vitro: Torkinib (PP242) potently inhibited mTOR (IC50: 8 nM) but was much less active against other PI3-K family members. Testing of this compound against 219 protein kinases revealed remarkable selectivity relative to the protein kinome. In BT549 cells, PP242 inhibited the phosphorylation of Akt, the mTOR substrate p70S6K, and its downstream target S6. PP242 suppressed growth by > 90%, with low nanomolar potency (GI50: 12 nM). PP242 had greater anti-proliferative potency relative to rapamycin in a panel of solid tumor cell lines carrying either PI3K gain-of-function or PTEN loss-of-function.

 

Melting Point: >187°C (dec.)

 

Boiling Point: 642.0±50.0 °C(Predicted)

 

Flash Point: 342.097℃

 

pKa: 9.51±0.40(Predicted)

 

Solubility: Soluble in DMSO; Insoluble in Water; Insoluble in Ethanol.

 

Isomeric SMILES: CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(N3)C=CC(=C4)O)N  

 

InChIKey: MFAQYJIYDMLAIM-UHFFFAOYSA-N  

 

InChI: InChI=1S/C16H16N6O/c1-8(2)22-16-13(15(17)18-7-19-16)14(21-22)12-6-9-5-10(23)3-4-11(9)20-12/h3-8,20,23H,1-2H3,(H2,17,18,19) 

 

Attribute
[Chem Name]	2-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol
[Synonym]	Torkinib; PP242
[CAS No.]	1092351-67-1
[MDL No.]	MFCD12196869
[Formula]	C16H16N6O
[Molecular]	308.34
[Form]	White powder
[Storage]	Keep in dark place. Inert atmosphere, 2-8°C

Goods Tag