PF-3758309

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Clon N/A
Menge 50mg
ArtNr HY-13007-50mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
PF 3758309, PF3758309
CAS No.
898044-15-0
Purity
>98%
MW
4906237
Formula
C25H30N8OS
Solubility
10 mM in DMSO
Biological Description
PF-3758309 is an inhbitor of PAK with IC50 of 1.3 nM for PAK4.
IC50 & Target: IC50: 1.3 nM (PAK4)
In Vitro: F-3758309 binds directly to PAK4 with an in vitro potency of 2.7-4.5 nM. PF-3758309 has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, Ki=18.1+/-5.1 nM; PAK6, Ki=17.1+/-5.3 nM) and group A PAK1 (Ki=13.7+/-1.8 nM), but is less active against the other two group A PAKs (PAK2, IC50=190 nM; PAK3, IC50=99 nM). PAK4 phosphorylates GEF-H1 on a previously characterized serine residue 810 and is inhibited by PF-3758309 (IC50=1.3+/-0.5 nM). PF-3758309 also inhibits endogenous pGEF-H1 accumulation in HCT116 cells[1]. PF-3758309 is profiled for its growth-inhibitory activity in a panel of 92 tumor cell lines, half of which exhibits IC50 values of less than 10 nM[2]. The proliferation of A549 cells is affected at the treatment with lower dosage (1 uM) of PF-3758309[3].
In Vivo: PF-3758309 (7.5-30 mg/kg BID, p.o.) results in statistically significant tumor growth inhibition (TGI) in five models including HCT116 and A549 models. PF-3758309 (15 mg/kg BID, p.o.) is found to inhibit [3H]FLT uptake 32.5% in the HCT116 tumor xenografts by day 6. PF-3758309 treatment shows a significant increase in the apoptotic marker activated caspase 3 in HCT116 tumors[1]. PF-3758309 (25 mg/kg, p.o.) exhibits antiproliferative effects on cell line xenografts[4].
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Sicherheitsdatenblatt

HY-13007-50mg.pdf

Menge: 50mg
Lieferbar: In stock
Listenpreis: 330,71 €
Rabatt: -10,0%
Preis: 297,64 €
Sie sparen: 33,07 €
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