PF-3758309
Synonym(s):p21-Activated Kinase Inhibitor II, PF-3758309 - CAS 898044-15-0 - Calbiochem;PAK Inhibitor II, PF3758309, ( S)-N-(2-(Dimethylamino)-1-phenylethyl)-6,6-dimethyl-3-(2-methylthieno[3,2-d]pyrimidin-4-ylamino)-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide;PAK Inhibitor II, PF3758309, (S)-N-(2-(Dimethylamino)-1-phenylethyl)-6,6-dimethyl-3-(2-methylthieno[3,2-d]pyrimidin-4-ylamino)-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide
- CAS NO.:898044-15-0
- Empirical Formula: C25H30N8OS
- Molecular Weight: 490.62
- MDL number: MFCD18633226
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-19 20:33:22
What is PF-3758309?
The Uses of PF-3758309
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.
Properties of PF-3758309
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 |
pka | 12.82±0.40(Predicted) |
form | Yellowish-white powder |
color | White to light yellow |
Safety information for PF-3758309
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H317:Sensitisation, Skin |
Precautionary Statement Codes |
P280:Wear protective gloves/protective clothing/eye protection/face protection. |
Computed Descriptors for PF-3758309
New Products
4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-(Dimethylamino)tetrahydro-2H-pyran-4-carbonitrile 4-Aminotetrahydropyran-4-carbonitrile Hydrochloride (R)-3-Aminobutanenitrile Hydrochloride 3-((Dimethylamino)methyl)-5-methylhexan-2-one oxalate 1,4-Dioxa-8-azaspiro[4.5]decane 5-Bromo-2-nitropyridine Nimesulide BP Aceclofenac IP/BP/EP Diclofenac Sodium IP/BP/EP/USP Mefenamic Acid IP/BP/EP/USP Ornidazole IP Diclofenac Potassium THOMAIND PAPER PH 2.0 TO 4.5 1 BOX BUFFER CAPSULE PH 9.2 - 10 CAP SODIUM CHLORIDE 0.1N CVS ALLOXAN MONOHYDRATE 98% PLATINUM 0.5% ON 3 MM ALUMINA PELLETS (TYPE 73) LITHIUM AAS SOLUTION 2-Bromo-1-(bromomethyl)-3-chloro-5-nitrobenzene 2-Bromo-3-nitroaniline N-(3-Hydroxypropyl)-N-methylacetamide 3-Bromo-6-chloropyridazine 4-ethyl-3-nitrobenzoic acidRelated products of tetrahydrofuran
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