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, 10 mM in DMSO
- CBNumber:
- CB92518269
- Molecular Formula:
- C16H16N6O
- Molecular Weight:
- 308.34
- MDL Number:
- MFCD12196869
- MOL File:
- 1092351-67-1.mol
- MSDS File:
- SDS
| Product description | Number | Pack Size | Price |
| PP242 ≥95% | 13643 | 1mg | $32 |
| PP242 ≥95% | 13643 | 5mg | $82 |
| PP242 ≥95% | 13643 | 10mg | $133 |
| PP242 | 13643 | 25mg | $290 |
| PP242 ≥98%(HPLC) | 4257 | 25 | $514 |
| More product size | |||
| 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
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H315-H319-H335 |
| Precautionary statements | P264-P280-P302+P352-P321-P332+P313-P362-P305+P351+P338-P337+P313-P261-P271-P304+P340-P312-P403+P233-P405-P501 |
| 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 |
PP242 Chemical Properties,Uses,Production
Description
The mammalian target of rapamycin (mTOR) is a serine-
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
References
[1] BETH APSEL. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases[J]. Nature chemical biology, 2008, 4 11: 691-699. DOI: 10.1038/nchembio.117
[2] MORRIS E FELDMAN. Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2.[J]. PLoS Biology, 2009, 7 2: e38. DOI: 10.1371/journal.pbio.1000038
[3] FUMIAKI KOJIMA . Prostaglandin E2 activates Rap1 via EP2/EP4 receptors and cAMP-signaling in rheumatoid synovial fibroblasts: Involvement of Epac1 and PKA[J]. Prostaglandins & other lipid mediators, 2009, 89 1: Pages 26-33. DOI: 10.1016/j.prostaglandins.2009.03.001
[4] MATTHEW R JANES. Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor[J]. Nature Medicine, 2010, 16 2: 205-213. DOI: 10.1038/nm.2091
PP242 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Capot Chemical Co.,Ltd. | +86-（0）57185586718; +8613336195806 | sales@capot.com | China | 29734 | 60 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | sales@coreychem.com | China | 29852 | 58 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 965 | 58 |
| Shenzhen Nexconn Pharmatechs Ltd | +86-755-89396905 +86-15013857715 | admin@nexconn.com | China | 10405 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19552 | 58 |
| Alchem Pharmtech,Inc. | 8485655694 | sales@alchempharmtech.com | United States | 63687 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49975 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32434 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
