Pyrrolo[3,4-c]pyrazole-5(1H)-carboxaMide, N-[(1S)-2-(diMethylaMino)-1-phenylethyl]-4,6-dihydro-6,6-diMethyl-3-[(2-Methylthieno[3,2-d]pyriMidin-4-yl)aMino]-
PF-3758309
CAS: 898044-15-0
Molecular Formula: C25H30N8OS
Pyrrolo[3,4-c]pyrazole-5(1H)-carboxaMide, N-[(1S)-2-(diMethylaMino)-1-phenylethyl]-4,6-dihydro-6,6-diMethyl-3-[(2-Methylthieno[3,2-d]pyriMidin-4-yl)aMino]- - Names and Identifiers
Pyrrolo[3,4-c]pyrazole-5(1H)-carboxaMide, N-[(1S)-2-(diMethylaMino)-1-phenylethyl]-4,6-dihydro-6,6-diMethyl-3-[(2-Methylthieno[3,2-d]pyriMidin-4-yl)aMino]- - Physico-chemical Properties
| Molecular Formula | C25H30N8OS |
| Molar Mass | 490.62 |
| Density | 1.325±0.06 g/cm3(Predicted) |
| Appearance | Yellowish-white powder |
| pKa | 12.82±0.40(Predicted) |
| Storage Condition | -20C |
| In vitro study | PF-3758309 was a potent (Kd = 2.7 nM),ATP competitive PAK4 inhibitor with a Ki of 18.7 nM. In cells, PF-3758309 inhibited the phosphorylation of PAK4 matrix GEF-H1 (IC50=1.3 nM) and the Anchorage-independent growth of tumor cell lines (IC50=4.7 nM). PF-3758309 also inhibited the accumulation of endogenous pGEF-H1 in HCT116 cells. PF-3758309 can effectively inhibit the differentiation (IC50=20 nM) and Anchorage Independent growth (IC50=27 nM) of A549 cells. PF-3758309 is a potent (K d = 2.7 nM) ATP competitive PAK4 inhibitor with K I of 18.7 nM. In cells, PF-3758309 inhibited the phosphorylation of PAK4 matrix GEF-H1 (IC50=1.3 nM) and the Anchorage-independent growth of tumor cell lines (IC50=4.7 nM). PF-3758309 also inhibited the accumulation of endogenous pGEF-H1 in HCT116 cells. PF-3758309 can effectively inhibit the differentiation (IC50=20 nM) and Anchorage Independent growth (IC50=27 nM) of A549 cells. |
| In vivo study | PF-3758309 blocking the growth of a variety of human tumor xenografts, the plasma EC50 value was 0.4 nM in most sensitive models. In the HCT116 tumor model, PF-3758309 was able to resist proliferation and induce apoptosis. PF-3758309 blocked the growth of multiple human tumor xenografts, with a plasma EC50 value of 0.4 nM in most sensitive models. In the HCT116 tumor model, PF-3758309 was able to resist proliferation and induce apoptosis. |
Pyrrolo[3,4-c]pyrazole-5(1H)-carboxaMide, N-[(1S)-2-(diMethylaMino)-1-phenylethyl]-4,6-dihydro-6,6-diMethyl-3-[(2-Methylthieno[3,2-d]pyriMidin-4-yl)aMino]- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.038 ml | 10.191 ml | 20.382 ml |
| 5 mM | 0.408 ml | 2.038 ml | 4.076 ml |
| 10 mM | 0.204 ml | 1.019 ml | 2.038 ml |
| 5 mM | 0.041 ml | 0.204 ml | 0.408 ml |
Last Update：2024-01-02 23:10:35
![Pyrrolo[3,4-c]pyrazole-5(1H)-carboxaMide, N-[(1S)-2-(diMethylaMino)-1-phenylethyl]-4,6-dihydro-6,6-diMethyl-3-[(2-Methylthieno[3,2-d]pyriMidin-4-yl)aMino]-](http://res.chembk.com/assets/images/structure/311621.gif)
Supplier List
Spot supply
Product Name: PF-3758309 Visit Supplier Webpage Request for quotationCAS: 898044-15-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: PF-3758309 Visit Supplier Webpage Request for quotationCAS: 898044-15-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History