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| | 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 | | EINECS: | | | 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 | | InChIKey | RYYNGWLOYLRZLK-RBUKOAKNSA-N | | SMILES | FC(F)(F)c1c(nc(nc1)Nc3cc4c(cc3)[C@H]5N([C@@H]4CC5)C(=O)CNC(=O)C)NC2CCC2 |
| WGK Germany | 3 | | Storage Class | 11 - Combustible Solids |
| | 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-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 | 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. |
| | PF-03814735 Preparation Products And Raw materials |
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