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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
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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].

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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PF-3758309 Suppliers

A.J Chemicals
Tel
--
Fax
--
Email
sales@ajchem.in
Country
India
ProdList
6100
Advantage
58
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View Lastest Price from PF-3758309 manufacturers

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:


  • 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
  • 898044-15-0
  • C25H30N8OS
  • Inhibitors