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PP242

PP242 Struktur
1092351-67-1
CAS-Nr.
1092351-67-1
Englisch Name:
PP242
Synonyma:
PP242;CS-19;Torkinib;PP242, >=98%;PP242;PP-242;PP242 USP/EP/BP;PP242 (Torkinib);Torkinib (PP242);PP242, Free Base;TORKINIB;PP242; PP-242;PP 242
CBNumber:
CB92518269
Summenformel:
C16H16N6O
Molgewicht:
308.34
MOL-Datei:
1092351-67-1.mol

PP242 Eigenschaften

Schmelzpunkt:
>187°C (dec.)
Siedepunkt:
642.0±50.0 °C(Predicted)
Dichte
1.55
Flammpunkt:
342.097℃
storage temp. 
-20°C Freezer, Under inert atmosphere
L?slichkeit
DMSO (Slightly), Methanol (Slightly, Sonicated)
Aggregatzustand
White powder solid.
pka
9.51±0.40(Predicted)
Farbe
Pale Brown to Light Brown

Sicherheit

HS Code  29339900

PP242 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

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.

Verwenden

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.

Enzyminhibitor

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.

PP242 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


PP242 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 173)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Capot Chemical Co.,Ltd.
+86-(0)57185586718 +86-13336195806
sales@capot.com China 29791 60
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 32951 60
career henan chemical co
+86-0371-86658258 +8613203830695
sales@coreychem.com China 29885 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 965 58
Shenzhen Nexconn Pharmatechs Ltd
+86-755-89396905 +86-15013857715
admin@nexconn.com China 10310 58
BOC Sciences
+1-631-485-4226
inquiry@bocsci.com United States 19553 58
Chongqing Chemdad Co., Ltd
+86-023-6139-8061 +86-86-13650506873
sales@chemdad.com China 39894 58
Alchem Pharmtech,Inc.
8485655694
sales@alchempharmtech.com United States 63687 58
CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 49374 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 32072 58

  • PP242
  • 2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol
  • PP242, Free Base
  • Torkinib
  • 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
  • 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
  • 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
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