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ChemicalBook >> CAS DataBase List >>PF-3758309

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;PF-3758309, 10 mM in DMSO;p21-Activated Kinase Inhibitor II, PF-3758309
CBNumber:
CB32624276
Molecular Formula:
C25H30N8OS
Molecular Weight:
490.62
MDL Number:
MFCD18633226
MOL File:
898044-15-0.mol
MSDS File:
SDS
Last updated:2025-04-17 18:22:24

PF-3758309 Properties

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
FDA UNII PK459EA5I2
UNSPSC Code 12352200

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H317
Precautionary statements  P280
NFPA 704
0
2 0

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
Product number Packaging Price Buy
5.00613 5mg $273 Buy
19186 5mg $62 Buy
19186 10mg $104 Buy
19186 25mg $239 Buy
KIN0000780 10MG $240.45 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].

IC 50

PAK4: 18.7 nM (Ki); PAK1: 13.7 nM (Ki); PAK5: 18.1 nM (Ki); PAK6: 17.1 nM (Ki); PAK2: 190 nM (IC50); PAK3: 99 nM (IC50); PAK4: 2.7 nM (Kd)

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

Global( 95)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 33024 60
career henan chemical co 		+86-0371-86658258 +8613203830695 factory@coreychem.com China 29808 58
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 32159 58
Dideu Industries Group Limited 		+86-29-89586680 +86-15129568250 1026@dideu.com China 22858 58
Zhejiang J&C Biological Technology Co.,Limited 		+1-2135480471 +1-2135480471 sales@sarms4muscle.com China 10473 58
InvivoChem 		+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6391 58
TargetMol Chemicals Inc. 		support@targetmol.com United States 38630 58
Wuhan Topule Biopharmaceutical Co., Ltd 		+8618327326525 masar@topule.com China 8467 58
LEAPCHEM CO., LTD. 		+86-852-30606658 market18@leapchem.com China 43340 58
Aladdin Scientific 		tp@aladdinsci.com United States 57505 58

View Lastest Price from PF-3758309 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
PF-3758309 pictures 2024-11-19 PF-3758309
898044-15-0
 US $55.00-145.00 / mg 99.37% 10g TargetMol Chemicals Inc.
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 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
  • PF-3758309 pictures
  • PF-3758309
    898044-15-0
  • US $55.00-145.00 / mg
  • 99.37%
  • TargetMol Chemicals Inc.

PF-3758309 Spectrum

PF-3758309 (S)-N-(2-(diMethylaMino)-1-phenylethyl)-6,6-diMethyl-3-((2-Methylthieno[3,2-d]pyriMidin-4-yl)aMino)-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxaMide PF-03758309/PF03758309 N-[(1S)-2-(Dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide PF-03758309 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]- N-[(1S)-2-(Dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide PF 3758309 X4Z N-[(1S)-2-(Dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl (S)-N-(2-(Dimethylamino)-1-phenylethyl)-6,6-dimethyl-3-((2-methylthieno[3,2-d]pyrimidin-4-yl)a CS-1014 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 p21-Activated Kinase Inhibitor II, PF-3758309 - CAS 898044-15-0 - Calbiochem PF 3758309;PF3758309 PF-309 PF-3758309 USP/EP/BP proliferation,tumor,PF-3758309,oncogenic,survival,PF03758309,PF3758309,inhibit,p21 activated kinases,signaling,Apoptosis,ATP-competitive,Inhibitor,PF 03758309,growth,PAK PF-3758309, 10 mM in DMSO p21-Activated Kinase Inhibitor II, PF-3758309 898044-15-0 C25H30N8OS Inhibitors