ChemicalBook > CAS DataBase List > PP242

PP242

Product Name
PP242
CAS No.
1092351-67-1
Chemical Name
PP242
Synonyms
CS-19;PP242;Torkinib;PP242, >=98%;PP242;PP-242;PP242 USP/EP/BP;PP242 (Torkinib);PP242, Free Base;Torkinib (PP242);TORKINIB;PP242; PP-242;PP 242
CBNumber
CB92518269
Molecular Formula
C16H16N6O
Formula Weight
308.34
MOL File
1092351-67-1.mol
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PP242 Property

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
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Safety

HS Code 
29339900
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
13643
Product name
PP242
Purity
≥95%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
13643
Product name
PP242
Purity
≥95%
Packaging
5mg
Price
$82
Updated
2024/03/01
Cayman Chemical
Product number
13643
Product name
PP242
Purity
≥95%
Packaging
10mg
Price
$133
Updated
2024/03/01
Cayman Chemical
Product number
13643
Product name
PP242
Packaging
25mg
Price
$290
Updated
2024/03/01
Tocris
Product number
4257
Product name
PP242
Purity
≥98%(HPLC)
Packaging
25
Price
$514
Updated
2021/12/16
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PP242 Chemical Properties,Usage,Production

Description

The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin) and regulate different pathways. PP242 is an inhibitor of the active site of mTOR kinase in both mTORC1 and mTORC2 (IC50 = 8 nM). It less effectively inhibits PKCα, PI3-kinase subunit p110γ, JAK2, PKCβI, and PKCβII (IC50 = 49, 102, 110, 198, and 185, respectively). PP242 has been shown to cause the death of certain human and murine leukemia cells more potently than rapamycin and, in vivo, delays leukemia onset and augments the effects of tyrosine kinase inhibitors in suppressing leukemic expansion and extending survival.

Uses

PP 242 is used in leukemia therapy suppressing mTOR signaling. Dual mTORC1/C2 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

PP242 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from PP242 manufacturers

Career Henan Chemical Co
Product
PP242 1092351-67-1
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-24

1092351-67-1, PP242Related Search:

PP1 PP2 USP/EP/BP Y27632 (hydrochloride) AZD-8055 MK-2206 2HCl WORTMANNIN Torin 1 Rapamycin

  • PP242
  • 2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol
  • PP242, Free Base
  • Torkinib
  • PP242 (Torkinib)
  • TORKINIB;PP242; PP-242;PP 242
  • CS-19
  • (2E)-2-(4-amino-1-propan-2-yl-2H-pyrazolo[3,4-d]pyrimidin-3-ylidene)indol-5-ol
  • 1H-Indol-5-ol, 2-[4-aMino-1-(1-Methylethyl)-1H-pyrazolo[3,4-d]pyriMidin-3-yl]-
  • Torkinib (PP242)
  • 2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol PP 242
  • PP242, >=98%
  • pp242, 2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol
  • PP242;PP-242
  • 2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol/PP242
  • PP242 USP/EP/BP
  • PP242 mTOR inhibitor ab141405 PP-242
  • 1092351-67-1
  • Akt
  • mTOR
  • PI3K
  • Inhibitors
  • Antineoplastic
  • PI3K/Akt/mTOR