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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >Cytoskeletal Signaling >PAK inhibitors >PF-3758309

PF-3758309

PF-3758309 Structure
  • ₹23250
  • Product name: PF-3758309
  • CAS: 898044-15-0
  • MF: C25H30N8OS
  • MW: 490.62
  • EINECS:
  • MDL Number:MFCD18633226
  • Synonyms: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
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Brand

  • Sigma-Aldrich(India)

Package

  • 5MG
  • ManufacturerSigma-Aldrich(India)
  • Product number5.00613
  • Product descriptionp21-Activated Kinase Inhibitor II, PF-3758309 - CAS 898044-15-0 - Calbiochem p21-Activated Kinase Inhibitor II, PF-3758309, CAS 898044-15-0, is a cell-permeable, reversible, potent inhibitor of p21-activated kinases (IC50 = 190
  • Packaging5MG
  • Price₹23250
  • Updated2022-06-14
  • Buy
Manufacturer Product number Product description Packaging Price Updated Buy
Sigma-Aldrich(India) 5.00613 p21-Activated Kinase Inhibitor II, PF-3758309 - CAS 898044-15-0 - Calbiochem p21-Activated Kinase Inhibitor II, PF-3758309, CAS 898044-15-0, is a cell-permeable, reversible, potent inhibitor of p21-activated kinases (IC50 = 190 5MG ₹23250 2022-06-14 Buy

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

Safety Information

Symbol(GHS): GHS hazard pictograms
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning GHS hazard pictograms P264, P270, P301+P312, P330, P501
H317 May cause an allergic skin reaction Sensitisation, Skin Category 1 Warning GHS hazard pictograms P261, P272, P280, P302+P352,P333+P313, P321, P363, P501
Precautionary statements:
P280 Wear protective gloves/protective clothing/eye protection/face protection.

Description

p21-Activated kinases (PAKs) are STE20 serine/threonine kinases that are vital to normal cell function. Binding of various upstream partners to PAKs results in release of an autoinhibitory domain that blocks activity of the kinase domain. PAKs are upregulated in several human cancers and are potential therapeutic targets for cancer intervention. PF-3758309 is an ATP-competitive inhibitor of PAK4, preventing the phosphorylation of the PAK4 substrate GEF-H1 (IC50 = 1.3 nM) and blocking anchorage-independent growth of a panel of tumor cell lines (IC50 = 4.7 nM). It also inhibits the ability of kinase domains from other PAKs to phosphorylate peptide substrates (Kis = 18.1, 17.1, 13.7, 190, and 99 nM for PAKs 5, 6, 1, 2, and 3, respectively). PF-3758309 blocks the growth of multiple human tumor xenografts.

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