898044-15-0
PF-3758309
CAS: 898044-15-0
Molecular Formula: C25H30N8OS
898044-15-0 - Names and Identifiers
898044-15-0 - 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. |
898044-15-0 - 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
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Product Name: PF-3758309 Request for quotationCAS: 898044-15-0
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Mobile: 18916960931
QQ: 3623107365
Wechat: 18916960931
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Product Name: PF-3758309 Visit Supplier Webpage Request for quotationCAS: 898044-15-0
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: PF-03758309 Visit Supplier Webpage Request for quotationCAS: 898044-15-0
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: PF-3758309 Visit Supplier Webpage Request for quotationCAS: 898044-15-0
Tel: 18301782025
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View History
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