PF-3758309
- CAS No.
- 898044-15-0
- Chemical Name:
- PF-3758309
- Synonyms
- X4Z;PF-309;CS-1014;PF-3758309;PF-03758309;PF 3758309;PF3758309;PF-3758309 USP/EP/BP;PF-03758309/PF03758309;p21-Activated Kinase Inhibitor II, PF-3758309 - CAS 898044-15-0 - Calbiochem;N-[(1S)-2-(Dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl
- CBNumber:
- CB32624276
- Molecular Formula:
- C25H30N8OS
- Molecular Weight:
- 490.62
- MDL Number:
- MFCD18633226
- MOL File:
- 898044-15-0.mol
- MSDS File:
- SDS
| Density | 1.325±0.06 g/cm3(Predicted) |
|---|---|
| storage temp. | -20C |
| solubility | ≥24.53 mg/mL in DMSO; insoluble in H2O; ≥101.4 mg/mL in EtOH with gentle warming and ultrasonic |
| form | Yellowish-white powder |
| pka | 12.82±0.40(Predicted) |
| FDA UNII | PK459EA5I2 |
PF-3758309 price More Price(21)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | 5.00613 | p21-Activated Kinase Inhibitor II, PF-3758309 - CAS 898044-15-0 - Calbiochem | 898044-15-0 | 5mg | $273 | 2023-01-07 | Buy |
| Cayman Chemical | 19186 | PF-3758309 ≥98% | 898044-15-0 | 5mg | $62 | 2024-03-01 | Buy |
| Cayman Chemical | 19186 | PF-3758309 ≥98% | 898044-15-0 | 10mg | $104 | 2024-03-01 | Buy |
| Cayman Chemical | 19186 | PF-3758309 ≥98% | 898044-15-0 | 25mg | $239 | 2024-03-01 | Buy |
| American Custom Chemicals Corporation | KIN0000780 | PF-3758309 95.00% | 898044-15-0 | 10MG | $240.45 | 2021-12-16 | Buy |
PF-3758309 Chemical Properties,Uses,Production
Uses
PF-3758309 is a pyrrolopyrazole inhibitor of PAK4 (p21-activated kinase). It is used in biological studies for targeting Rho GTPase signaling for cancer therapy.
Definition
ChEBI: N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methyl-4-thieno[3,2-d]pyrimidinyl)amino]-1,4-dihydropyrrolo[3,4-c]pyrazole-5-carboxamide is an organic heterobicyclic compound, an organosulfur heterocyclic compound and an organonitrogen heterocyclic compound.
Biological Activity
pf-3758309 is an inhbitor of pak4 with ic50 of 1.3 nm [1].p21-activated kinases (paks) are the family of serine/theronine kinases, which play important role in linking rho gtpase to cytoskeleton reorganization and nuclear signaling. pak4 is a member of paks family, specifically responsive for interacting with gtp bound form of cdc42 and jnk family. pak4 is involved in filopodia formation and may play a role in the reorganization of the actin cytoskeleton.biochemical study had identified that pf-3758309 was an atp-competitive inhibitor of pak4, which inhibited the kinase activity [1]. when pak4 was screened with a panel of tumor cell lines, it was found pf-3758309 inhibited the phosphorylation of pak4 substrate gef-h1, and also the pak4-induced anchorage-independent cell growth, with ic50 value of 1.3 nm and 4.7 ±3 nm respectively [1]. when pf-3758309 was screened with a panel of paks related kinases, it exhibited good potency and specificity for pak4 [1]. cell analysis confirmed that pf-3758309 modulates pak4-dependent signaling nodes and identifies unexpected links to additional p53pathways [1].
in vivo
activity of pf-3758309 was examined in a panel of human xenograft model, including hct116 and a549 model. twice daily oral administration of pf-3758309 (7.5-30 mg/kg bid) for 9-18 days resulted in significant inhibition of tumor growth in all the models. the tumor growth was shown to be caused by pak-dependent pathways in hct116 and a549 model. additionally, pf-3758309 was shown to regulate pak-associated cell proliferation and survival in certain models. therefore, pf-3758309 exhibited inhibitory activity on pak4 [1].
References
[1] murray b w et al. , small-molecule p21-activated kinase inhibitor pf-3758309 is a potent inhibitor of oncogenic signaling and tumor growth. proc natl acad sci usa. 2010, 107(20): 9446-9451.
PF-3758309 Preparation Products And Raw materials
Raw materials
Preparation Products
PF-3758309 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29118 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43348 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |
View Lastest Price from PF-3758309 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
![N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-1,4-dihydropyrrolo[3,4-c]pyrazole-5-carboxamide pictures](https://img.chemicalbook.com/ProductImageEN/2020-1/Small/fa88ef0b-eaac-444c-8fd5-01ae34e6aa38.png) |
2020-01-02 | N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-1,4-dihydropyrrolo[3,4-c]pyrazole-5-carboxamide
898044-15-0
|
US $1.00 / KG | 1KG | Min98% HPLC | g/kg/ton | Career Henan Chemical Co |
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- N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-1,4-dihydropyrrolo[3,4-c]pyrazole-5-carboxamide
898044-15-0
- US $1.00 / KG
- Min98% HPLC
- Career Henan Chemical Co