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ChemicalBook--->CAS DataBase List--->942487-16-3

942487-16-3

942487-16-3 Structure

942487-16-3 Structure
IdentificationBack Directory
[Name]

PF-03814735
[CAS]

942487-16-3
[Synonyms]

CS-240
PF-03814735
PF-03814735 USP/EP/BP
RYYNGWLOYLRZLK-RBUKOAKNSA-N
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]-
[Molecular Formula]

C23H25F3N6O2
[MDL Number]

MFCD16659065
[MOL File]

942487-16-3.mol
[Molecular Weight]

474.48
Chemical PropertiesBack Directory
[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
Safety DataBack Directory
[WGK Germany ]

3
Hazard InformationBack Directory
[Description]

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 HCT116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT116 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.
[Chemical Properties]

Off-White Solid
[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.
[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]
[storage]

Store at -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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