PF-3758309
- Product Name
- 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
- Formula Weight
- 490.62
- MOL File
- 898044-15-0.mol
PF-3758309 Property
- 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)
- color
- White to light yellow
N-Bromosuccinimide Price
- Product number
- 5.00613
- Product name
- p21-Activated Kinase Inhibitor II, PF-3758309 - CAS 898044-15-0 - Calbiochem
- Packaging
- 5mg
- Price
- $273
- Updated
- 2023/01/07
- Product number
- 19186
- Product name
- PF-3758309
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $62
- Updated
- 2024/03/01
- Product number
- 19186
- Product name
- PF-3758309
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $104
- Updated
- 2024/03/01
- Product number
- 19186
- Product name
- PF-3758309
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $239
- Updated
- 2024/03/01
- Product number
- KIN0000780
- Product name
- PF-3758309
- Purity
- 95.00%
- Packaging
- 10MG
- Price
- $240.45
- Updated
- 2021/12/16
PF-3758309 Chemical Properties,Usage,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
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View Lastest Price from PF-3758309 manufacturers
- Product
- 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
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- Min98% HPLC
- Supply Ability
- g/kg/ton
- Release date
- 2020-01-01