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ChemicalBook > Product Catalog >Biochemical Engineering >Inhibitors >PI3K / Akt / mTOR >mTOR inhibitors >PP242

PP242

PP242 Structure
CAS No.
1092351-67-1
Chemical Name:
PP242
Synonyms
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
Molecular Formula:
C16H16N6O
Molecular Weight:
308.34
MOL File:
1092351-67-1.mol
MSDS File:
SDS
Modify Date:
2023/6/30 15:45:59
Request For Quotation

PP242 Properties

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

Risk and Safety Statements

HS Code  29339900

PP242 Chemical Properties,Uses,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.

PP242 Preparation Products And Raw materials

Raw materials

Preparation Products

PP242 Suppliers

Global( 175)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
A.J Chemicals 91-9810153283 New Delhi, India 6124 58 Inquiry
CLEARSYNTH LABS LTD. +91-22-45045900 Hyderabad, India 6351 58 Inquiry
Capot Chemical Co.,Ltd. 571-85586718 +8613336195806 China 29798 60 Inquiry
ATK CHEMICAL COMPANY LIMITED +undefined-21-51877795 China 32760 60 Inquiry
career henan chemical co +86-0371-86658258 +8613203830695 China 29900 58 Inquiry
Shenzhen Nexconn Pharmatechs Ltd +86-755-89396905 +86-15013857715 China 10259 58 Inquiry
BOC Sciences +1-631-485-4226 United States 19553 58 Inquiry
Chongqing Chemdad Co., Ltd +86-023-6139-8061 +86-86-13650506873 China 39916 58 Inquiry
CONIER CHEM AND PHARMA LIMITED +8618523575427 China 49391 58 Inquiry
TargetMol Chemicals Inc. +1-781-999-5354 +1-00000000000 United States 19892 58 Inquiry
Supplier Advantage
A.J Chemicals 58
CLEARSYNTH LABS LTD. 58
Capot Chemical Co.,Ltd. 60
ATK CHEMICAL COMPANY LIMITED 60
career henan chemical co 58
Shenzhen Nexconn Pharmatechs Ltd 58
BOC Sciences 58
Chongqing Chemdad Co., Ltd 58
CONIER CHEM AND PHARMA LIMITED 58
TargetMol Chemicals Inc. 58

PP242 Spectrum

PP242(1092351-67-1)1HNMR

1092351-67-1(PP242)Related Search:

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