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PF-03814735

PF-03814735 ??? ???
?? ??:
942487-16-3
???:
PF-03814735
???(??):
CS-240;PF-03814735;Abecarr impurity 1;Abecarnil Impurity 3;PF-03814735 USP/EP/BP;PF-03814735 PF03814735;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]-
CBNumber:
CB02598705
???:
C23H25F3N6O2
??? ??:
474.48
MOL ??:
942487-16-3.mol
MSDS ??:
SDS

PF-03814735 ??

???
181-183°C
??
1.443
?? ??
-20°C
???
DMSO: ???20mg/mL, ??
??? ??
??
?? ?? (pKa)
15.02±0.46(Predicted)
??
???? ????
??
  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
WGK ?? 3
????(GHS): GHS hazard pictograms
?? ?: Warning
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H315 ??? ??? ??? ????? ?? ????? ?? 2 ?? GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 ?? ?? ??? ??? ?? ? ?? ?? ??? ?? ?? 2A ?? GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 ?? ???? ??? ? ?? ?? ???? ?? - 1? ??;???? ?? ?? 3 ?? GHS hazard pictograms
??????:
P261 ??·?·??·???·??·...·????? ??? ????.
P264 ?? ??? ?? ??? ????.
P264 ?? ??? ?? ??? ????.
P271 ?? ?? ??? ? ?? ???? ?????.
P280 ????/???/???/?????? ?????.
P302+P352 ??? ??? ??? ?? ????.
P305+P351+P338 ?? ??? ? ?? ?? ???? ????. ???? ?????? ?????. ?? ????.
P332+P313 ?? ??? ??? ???? ??· ??? ????.
P337+P313 ?? ?? ??? ???? ???? ??· ??? ????.
P362 ??? ??? ?? ?? ?? ?????
P403+P233 ??? ??? ? ?? ?? ??? ???? ?????.
P405 ???? ?????.
P501 ...? ??? / ??? ?? ???.

PF-03814735 C??? ??, ??, ??

??

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.

??? ??

Off-White Solid

??

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]

PF-03814735 ?? ?? ? ???

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PF-03814735 ?? ??

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??? ?? ??? ?? ?? ? ??
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