PF-03814735|cas 942487-16-3|DC Chemicals

Cas No.:	942487-16-3
Synonyms:	PF 03814735;PF03814735
SMILES:	O=C(CNC(C)=O)N1[C@@H]2C3=C(C=C(NC4=NC(NC5CCC5)=C(C(F)(F)F)C=N4)C=C3)[C@H]1CC2
Formula:	C₂₃H₂₅F₃N₆O₂
M.Wt:	474.4788
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

PF-03814735 is a novel, potent, orally bioavailable, reversible small-molecule Aurora kinase inhibitor with IC50 of 0.8, 5, 10 and 22 nM for Aurora A, Aurora B, Flt 1 and FAk, respectively. PF-03814735 possesses potential antineoplastic activity. Aurora kinase inhibitor PF-03814735 binds to and blocks Aurora kinases A and B, which may result in the prevention of cellular division and proliferation in tumor cells that overexpress these kinases. In intact cells, the preventive activity of PF-03814735 on the Aurora1 and Aurora2 kinases attenuates levels of phospho-Aurora1, phosphohistone H3, and phospho-Aurora2. PF-03814735 generates a block in cytokinesis, leading to prevention of cell proliferation and the formation of polyploid multinucleated cells. Although PF-03814735 generates significant prevention of several other protein kinases, the predominant biochemical effects in cellular assays are consistent with inhibition of Aurora kinases. Once-daily oral injection of PF-03814735 to mice bearing human xenograft tumors generates an attenuation in phosphohistone H3 in tumors at doses that are tolerable and that result in significant inhibition of tumor growth. The combination of PF-03814735 and docetaxel in xenograft mouse tumor models shows additive tumor growth inhibition.

Cat. No.	Product name	Field of application
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DC47247	Tyrosylleucine TFA	Tyrosylleucine (Tyr-Leu, YL) TFA, an orally active dipeptide, exhibits a potent antidepressant-like activity.
DC47243	Dehydroglyasperin C	Dehydroglyasperin C, a isoflavone, is a potent NAD(P)H:oxidoquinone reductase (NQO1) and phase 2 enzyme inducer. Dehydroglyasperin C has antioxidant, neuroprotective, cancer chemopreventive, and anti-inflammatory activities.
DC47227	(−)-Myrtenal	(−)-Myrtenal ((1R)-(−)-Myrtenal) is an orally active terpene with antitumour activity. (−)-Myrtenal ameliorates hyperglycemia by enhancing GLUT2 through Akt in the skeletal muscle and liver of diabetic rats.
DC47224	GPX4-IN-3	GPX4-IN-3 (26a) is a potent glutathione peroxidase 4 (GPX4) inhibitor as a selective ferroptosis inducer. GPX4-IN-3 (26a) exhibits 71.7% inhibition for GPX4 with 1 μM.
DC47179	Tyrosylleucine	Tyrosylleucine (Tyr-Leu, YL), an orally active dipeptide, exhibits a potent antidepressant-like activity.
DC47178	Mead acid	Mead acid (5,8,11-Eicosatrienoic acid), an unsaturated (Omega-9) fatty acid, is an indicator of essential fatty acid deficiency.
DC47140	Yadanzioside K	Yadanzioside K is a natural quassinoid glucoside found in Brucea amarissima.
DC47105	Complanatoside B	Complanatoside B is a P. chinense Fisch flavonoid with potential anti-inflammatory effects.