2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol
PP242
CAS: 1092351-67-1
Molecular Formula: C16H16N6O
2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol - Names and Identifiers
2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol - Physico-chemical Properties
| Molecular Formula | C16H16N6O |
| Molar Mass | 308.34 |
| Density | 1.55 |
| Melting Point | >187°C (dec.) |
| Boling Point | 642.0±50.0 °C(Predicted) |
| Flash Point | 342.097℃ |
| Solubility | DMSO (Slightly), Methanol (Slightly, Sonicated) |
| Appearance | White powder solid. |
| Color | Pale Brown to Light Brown |
| pKa | 9.51±0.40(Predicted) |
| Storage Condition | -20°C Freezer, Under inert atmosphere |
| Use | Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM; Targeted to mTOR complex, acting on mTOR is more than 10 times and 100 times higher than acting on PI3Kδ or PI3Kα/β/γ, respectively. |
| In vitro study | PP242 acts on mTOR more than other PI3K family kinases, such as p110α,p110β,p110γ,p110δ, and DNA-PK(IC50 is 1.96 μm, 2.2 μm, 1.27 μm, respectively, 0.102 μm, and 0.408 μm), showed more effective selectivity. PP242 exhibited some inhibitory activity against Ret,PKC α,PKC β, and JAK2, and showed significant selectivity against 215 other protein kinases. Unlike rapamycin,PP242 inhibits both mTORC1 and mTORC2. In BT549 cells, PP242 treatment (0.04-10 μm) inhibited phosphorylation of Akt, the mTOR substrate p70S6K, and its downstream target S6 in a dose-dependent manner. PP242 effectively inhibits PKC Alpha, IC50 is 49 nM. Low concentrations of PP242 inhibited Akt S473 phosphorylation, and higher concentrations partially inhibited Akt T308-P except S473-P. As a more potent inhibitor of mTORC1 than rapamycin, PP242 was able to inhibit the proliferation of primary MEFs cells, and the phosphorylation of 4EBP1 on T36/45 and S65 was more potent than rapamycin. By causing higher levels of 4EBP1 and eIF4E binding than rapamycin, PP242 effectively inhibits cap-dependent translation, whereas rapamycin has no such effect. PP242 potently inhibited the proliferation of p190-transformed mouse BM,SUP-B15, and K562 cells with GI50 values of 12 nM,90 nM, and 85 nM, respectively. PP242 also inhibits the growth of solid tumor cell lines such as SKOV3,PC 3,786-O, and U87, GI50 is 0.49 μ M,0.19 μ M,2.13 μ M, respectively, and 1.57 M. PP242 was able to cause multiple myeloma (MM) cell reduction and apoptosis more effectively than rapamycin. |
| In vivo study | In mouse fat and liver, PP242 administration was able to completely inhibit the phosphorylation of Akt at S473 and t308. PP242 only partially inhibited Akt phosphorylation in skeletal muscle and was more effective at inhibiting phosphorylation of T308 than S473, although it was able to completely inhibit phosphorylation of 4EBP1 and S6. Oral administration of PP242 effectively delayed the onset of leukemia in a mouse model and induced leukemia regression by inhibiting the activation of mTORC2 and mTORC1 associated with cell size loss. The PP242 treatment effectively inhibited the growth of 8226 cells in mice. |
2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol - Risk and Safety
| HS Code | 29339900 |
2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.243 ml | 16.216 ml | 32.432 ml |
| 5 mM | 0.649 ml | 3.243 ml | 6.486 ml |
| 10 mM | 0.324 ml | 1.622 ml | 3.243 ml |
| 5 mM | 0.065 ml | 0.324 ml | 0.649 ml |
Last Update：2024-01-02 23:10:35
2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol - Reference Information
| biological activity | Torkinib (PP242) is a selective inhibitor of mTOR, the IC50 was 8 nM in the cell-free assay; Targeting the mTOR complex with more than 10-fold and 100-fold higher selectivity to mTOR than to PI3Kδ or PI3Kα/β/γ, respectively. Torkinib (PP242) induces mitochondrial autophagy and apoptosis. |
| Target | Value |
| mTOR (Cell-free assay) | 8 nM |
| p110δ (Cell-free assay) | 0.10 μM |
| DNA-PK (Cell-free assay) | 0.41 μM |
| PDGFR (Cell-free assay) | 0.41 μM |
Last Update：2024-04-09 19:05:17
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Product Name: PP242 Visit Supplier Webpage Request for quotationCAS: 1092351-67-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol
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