PF-3758309
898044-15-0
0.98%
2026-08-21
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Product Description
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Seller Information
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Description
ProductName PF-3758309 Cat No CEI-1472 Description PF-03758309 is a potent, ATP-competitive, pyrrolopyrazole inhibitor of PAK4 with IC50 of 1.3 nM. Product Overview PF-3758309 is an inhbitor of PAK4 with IC50 of 1.3 nM. 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. 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. When PF-3758309 was screened with a panel of PAKs related kinases, it exhibited good potency and specificity for PAK4.Cell analysis confirmed that PF-3758309 modulates PAK4-dependent signaling nodes and identifies unexpected links to additional p53pathways. 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. CAS No 898044-15-0 Molecular Weight 490.62 Purity 0.98 Storage Store at -20°C Synonyms PF 3758309; PF3758309 Targets PAK4 IC50 Ki=18.7 nM, Kd = 2.7 nM Molecular Formula C25H30N8OS Chemical Name 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 Solubility Soluble in DMSO > 10 mM Shipping Conditions Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request category Inhibitors(c1514) cas_num 898044-15-0 Basic Info-
Product Name:
PF-3758309
Other Name: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)-carboxamidePF 3758309;X4Z
CAS No.:898044-15-0
Molecular Formula:C25H30N8OS
InChIKeys:AYCPARAPKDAOEN-LJQANCHMSA-N
Molecular Weight:490.6237
Exact Mass:490.226
UNII:PK459EA5I2
DSSTox ID:DTXSID70649389
Categories:
Characteristics-
PSA:
130
XLogP3:3.1
Density:1.325±0.06 g/cm3(Predicted)
Hazard IdentificationClassification of the substance or mixture
Acute toxicity - Category 3, Oral
GHS label elements, including precautionary statements
Pictogram(s) 
Signal word Danger
Hazard statement(s) H301 Toxic if swallowed
Precautionary statement(s) Prevention P264 Wash ... thoroughly after handling.
P270 Do not eat, drink or smoke when using this product.
Response P301+P316 IF SWALLOWED: Get emergency medical help immediately.
P321 Specific treatment (see ... on this label).
P330 Rinse mouth.
Storage P405 Store locked up.
Disposal P501 Dispose of contents/container to an appropriate treatment and disposal facility in accordance with applicable laws and regulations, and product characteristics at time of disposal.
Other hazards which do not result in classification
no data available
Handling and StoragePrecautions for safe handling
Handling in a well ventilated place. Wear suitable protective clothing. Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Use non-sparking tools. Prevent fire caused by electrostatic discharge steam.
Conditions for safe storage, including any incompatibilities
Store the container tightly closed in a dry, cool and well-ventilated place. Store apart from foodstuff containers or incompatible materials.
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Seller Information
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Business Type:
Manufactory
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Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Location:
Shirley, New York 11967, USA
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Payment Terms:
TT against copy of documents,D/P
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Average lead Time:
15
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Total Annual Revenue:
$1 million-$2.5 million
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Year of Establishment:
2004
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Country Product Purchase Quantity Date Posted Post an enquiry for this product