ChemicalBook > CAS DataBase List > PF-3758309

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;PF-3758309, 10 mM in DMSO;p21-Activated Kinase Inhibitor II, PF-3758309
CBNumber: CB32624276
Molecular Formula: C25H30N8OS
Formula Weight: 490.62
MOL File: 898044-15-0.mol

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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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H317May cause an allergic skin reaction

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

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N-Bromosuccinimide Price

Sigma-Aldrich

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

Cayman Chemical

Product number: 19186
Product name: PF-3758309
Purity: ≥98%
Packaging: 5mg
Price: $62
Updated: 2024/03/01

Cayman Chemical

Product number: 19186
Product name: PF-3758309
Purity: ≥98%
Packaging: 10mg
Price: $104
Updated: 2024/03/01

Cayman Chemical

Product number: 19186
Product name: PF-3758309
Purity: ≥98%
Packaging: 25mg
Price: $239
Updated: 2024/03/01

American Custom Chemicals Corporation

Product number: KIN0000780
Product name: PF-3758309
Purity: 95.00%
Packaging: 10MG
Price: $240.45
Updated: 2021/12/16

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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].

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

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View Lastest Price from PF-3758309 manufacturers

Ningbo Qingteng Plastic Cost.,Ltd.

Product: P21 898044-15-0
Price: US $10.00/box
Min. Order: 1box
Purity: 99%
Supply Ability: 100000box
Release date: 2025-09-05

Career Henan Chemical Co

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

898044-15-0, PF-3758309Related Search:

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PF-3758309

CS-1014

(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

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