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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PP242 Suppliers

China 149 India 2 Switzerland 1 United Kingdom 3 United States 19 Global 174

Shanghai Boyle Chemical Co., Ltd.

Tel
Fax: 86-21-57758967
Email: sales@boylechem.com
Country: China
ProdList: 2923
Advantage: 55

J & K SCIENTIFIC LTD.

Tel: 010-82848833 400-666-7788
Fax: 86-10-82849933
Email: jkinfo@jkchemical.com
Country: China
ProdList: 96815
Advantage: 76

Chembest Research Laboratories Limited

Tel: 021-20908456
Fax: 021-58180499
Email: sales@BioChemBest.com
Country: China
ProdList: 6011
Advantage: 61

JinYan Chemicals(ShangHai) Co.,Ltd.

Tel: 13817811078
Fax: 86-021-50426522,50426273
Email: sales@jingyan-chemical.com
Country: China
ProdList: 9984
Advantage: 60

Shangchem Co., Ltd.

Tel: +86-21-68182121
Fax: +86-21-68182121
Country: China
ProdList: 882
Advantage: 52

Chemsky (shanghai) International Co.,Ltd

Tel: 021-50135380
Email: shchemsky@sina.com
Country: China
ProdList: 15421
Advantage: 60

China DongFan Chemical Co.,LTD

Tel: 86-0571-85151182
Fax: 86-0571-85151182
Country: China
ProdList: 5700
Advantage: 66

Jinan Trio PharmaTech Co., Ltd.

Tel: +86 (531) 88811783
Fax: +86 (531) 55696010 QQ 1762738062
Email: sales@trio-pharmatech.com (International market)
Country: China
ProdList: 1856
Advantage: 62

Shanghai Sunway Pharmaceutical Technology Co., Ltd

Tel: +8618575662672 18575662672
Fax: 021 51613951
Email: mzeng@3wpharm.com
Country: China
ProdList: 9747
Advantage: 57

Dalian Meilun Biotech Co., Ltd.

Tel: 0411-62910999 13889544652
Email: sales@meilune.com
Country: China
ProdList: 4647
Advantage: 58

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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