PP242
- CAS NO.:1092351-67-1
- Empirical Formula: C16H16N6O
- Molecular Weight: 308.34
- MDL number: MFCD12196869
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-06 16:01:30
What is PP242?
Description
The mammalian target of rapamycin (mTOR) is a serine-
The Uses of PP242
PP 242 is used in leukemia therapy suppressing mTOR signaling. Dual mTORC1/C2 inhibitor.
What are the applications of Application
PP242 is a selective FRAP inhibitor
Definition
ChEBI: A member of the class of pyrazolopyrimidines that is 1H-pyrazolo[3,4-d]pyrimidine substituted by isopropyl, 5-hydroxyindol-2-yl and amino groups at positions 1, 3 and 4 respectively. It is a potent inhibitor of mTOR and exhi its anti-cancer properties.
Enzyme inhibitor
This ATP-competitive mTORC1/mTORC2 inhibitor (FW = 308.34 g/mol; CAS 1092351-67-1; Solubility: 25 mM in DMSO), also named 2-[4-amino- 1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol, has a IC50 = 8 nM for both isoforms of mammalian target of rapamycin (mTOR), also known as FK506-binding protein 12-rapamycin-associated protein 1, or FRAP1, a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, autophagy, and transcription. PP-242 shows considerable selectivity for mTOR versus PI3K family kinases. In models of acute leukemia harboring the Philadelphia chromosome (Ph) translocation, PP242, but not rapamycin, causes death of mouse and human leukemia cells. Indeed, PP242 completely inhibits TORC1 and TORC2 signaling in BCR-ABL+ cells, whereas rapamycin partially suppresses TORC1 and drives a PI3K/AKT surge. Moreover, PP242 augments TNF-related apoptosis-inducing ligand- (TRAIL-) induced apoptosis in NSCLC cells, indicating that mTORC2 regulates Cbl-dependent FLIPS degradation and TRAIL-induced apoptosis Other Targets: p110γ (IC50 = 0.102 μM); DNA-PK ((IC50 = 0.408 μM); p110δ ((IC50 = 1.27 μM); p110α ((IC50 = 1.96 μM), and p110β ((IC50 = 2.2 μM), with much weaker inhibition of 215 other kinases.
storage
Store at +4°C
Properties of PP242
Melting point: | >187°C (dec.) |
Boiling point: | 642.0±50.0 °C(Predicted) |
Density | 1.55 |
Flash point: | 342.097℃ |
storage temp. | -20°C Freezer, Under inert atmosphere |
solubility | DMSO (Slightly), Methanol (Slightly, Sonicated) |
form | White powder solid. |
pka | 9.51±0.40(Predicted) |
color | Pale Brown to Light Brown |
Safety information for PP242
Computed Descriptors for PP242
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