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PP242

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
MDL Number:
MFCD12196869
MOL File:
1092351-67-1.mol
MSDS File:
SDS
Last updated:2024-11-19 23:02:33

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
FDA UNII H5669VNZ7V

SAFETY

Risk and Safety Statements

HS Code  29339900

PP242 price More Price(48)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 13643 PP242 ≥95% 1092351-67-1 1mg $32 2024-03-01 Buy
Cayman Chemical 13643 PP242 ≥95% 1092351-67-1 5mg $82 2024-03-01 Buy
Cayman Chemical 13643 PP242 ≥95% 1092351-67-1 10mg $133 2024-03-01 Buy
Cayman Chemical 13643 PP242 1092351-67-1 25mg $290 2024-03-01 Buy
Tocris 4257 PP242 ≥98%(HPLC) 1092351-67-1 25 $514 2021-12-16 Buy
Product number Packaging Price Buy
13643 1mg $32 Buy
13643 5mg $82 Buy
13643 10mg $133 Buy
13643 25mg $290 Buy
4257 25 $514 Buy

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.

storage

Store at +4°C

PP242 Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 172)Suppliers
Supplier Tel Email Country ProdList Advantage
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 32957 60
career henan chemical co
+86-0371-86658258 +8613203830695 sales@coreychem.com China 29880 58
Biochempartner
0086-13720134139 candy@biochempartner.com CHINA 965 58
Shenzhen Nexconn Pharmatechs Ltd
+86-755-89396905 +86-15013857715 admin@nexconn.com China 10311 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 32161 58

View Lastest Price from PP242 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Torkinib pictures 2024-11-19 Torkinib
1092351-67-1
US $52.00-97.00 / mg 99.23% 10g TargetMol Chemicals Inc.
PP242 pictures 2019-07-06 PP242
1092351-67-1
US $2.00 / kg 1kg 99% 100kg Career Henan Chemical Co
  • Torkinib pictures
  • Torkinib
    1092351-67-1
  • US $52.00-97.00 / mg
  • 99.23%
  • TargetMol Chemicals Inc.
  • PP242 pictures
  • PP242
    1092351-67-1
  • US $2.00 / kg
  • 99%
  • Career Henan Chemical Co

PP242 Spectrum

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