PF-03814735
PF-03814735 Basic information
- Product Name:
- PF-03814735
- Synonyms:
-
- PF-03814735
- N-[2-[(1S,4R)-6-[[4-(Cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]acetamide
- Acetamide, N-[2-[(1S,4R)-6-[[4-(cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]-
- RYYNGWLOYLRZLK-RBUKOAKNSA-N
- CS-240
- PF-03814735 USP/EP/BP
- Abecarnil Impurity 3
- PF-03814735 PF03814735
- CAS:
- 942487-16-3
- MF:
- C23H25F3N6O2
- MW:
- 474.48
- Product Categories:
-
- Inhibitor
- Mol File:
- 942487-16-3.mol
PF-03814735 Chemical Properties
- Melting point:
- 181-183°C
- Density
- 1.443
- storage temp.
- -20°C
- solubility
- DMSO: soluble20mg/mL, clear
- form
- powder
- pka
- 15.02±0.46(Predicted)
- color
- white to beige
PF-03814735 Usage And Synthesis
Description
The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-
Chemical Properties
Off-White Solid
Uses
The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays. PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively. PF-03814735 inhibits cell proliferation of HCT-116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT-116 tumor xenograft mouse model. PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.[Cayman Chemical]
Uses
PF 03814735 is an orally bioavailable small molecule aurora kinase inhibitor that plays a key role in the regulation of mitosis. PF 03814735 is a anticancer agent used for cancer therapy.
in vivo
Once-daily oral administration of PF-03814735 to mice bearing human xenograft tumors produces a reduction 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[1]. PF-03814735 is much more effective in NCI-H82 xenografts when administered on a weekly dosing schedule at 80 mg/kg compared with a daily schedule at 15 mg/kg. PF-03814735 delayed growth by 23.5 days on the weekly schedule, which corresponds to 0.9 logs of net cell kill during the course of treatment[2].
IC 50
Aurora 1: 0.8 nM (IC50); Aurora 2: 5 nM (IC50); Flt-1: 10 nM (IC50); FAK: 22 nM (IC50); TrkA: 30 nM (IC50); Met: 100 nM (IC50); FGFR1: 100 nM (IC50)
storage
-20°C
References
[1] jani jp, arcari j, bernardo v, bhattacharya sk, briere d, cohen bd, coleman k, christensen jg, emerson eo, jakowski a, hook k, los g, moyer jd, pruimboom-brees i, pustilnik l, rossi am, steyn sj, su c, tsaparikos k, wishka d, yoon k, jakubczak jl. pf-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. mol cancer ther. 2010 apr;9(4):883-94.
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