| Cat.No.: | BSM-0021 |
| Product Name: | PF-03814735 |
| CAS No.: | 942487-16-3 |
| Description: | PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. |
| Molecular Weight: | 474.48 |
| Storage: | 2 years -20°C Powder; 2 weeks 4°C in DMSO; 6 months -80°C in DMSO. |
| Targets: | Aurora A, Aurora B, Flt1, FAK, TrkA |
| IC50: | 0.8 nM; 5 nM; 10 nM; 22 nM; 30 nM |
| Molecular Formula: | C23H25F3N6O2 |
| Chemical Name: | 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]- |
| Solubility: | DMSO 0.4 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL |
| In Vitro: | In intact cells, the inhibitory activity of PF-03814735 on the Aurora1 and Aurora2 kinases reduces levels of phospho-Aurora1 (Thr 232, a sensitive marker of Aurora1 activity, with IC50 ~ 20 nM), phosphohistone H3 (with IC50 ~ 50 nM), and phospho-Aurora2 (with IC50 ~150 nM). PF-03814735 produces a block in cytokinesis, resulting in inhibition of cell proliferation and the formation of polyploid multinucleated cells. A recent research indicates small cell lung cancer (SCLC) and, to a lesser extent, colon cancer lines are very sensitive to PF-03814735. The status of the Myc gene family and retinoblastoma pathway members significantly correlates with the efficacy of PF-03814735. |
| In Vivo: | Once-daily oral dosing of >20 mg/kg of PF-03814735 for 10 days to mice bearing HCT-116 xenografts resulted in statistically significant and dose-dependent tumor growth inhibition of >50% relative to vehicle-treated mice. The inhibition is associated with a reduction in phosphorylated histone H3 levels. Significant single-agent antitumor efficacy is observed in five additional xenograft tumor models, including A2780 ovarian carcinoma, MDA-MB-231 breast carcinoma, colo-205 and SW620 colorectal carcinomas, and HL-60 acute promyelocytic leukemia. In vivo experiments with two SCLC xenograft models confirms the sensitivity of Myc gene-driven models to PF-03814735 and a possible schedule dependence of MYC/c-Myc-driven tumors. |
| Warning: | For Research Use Only! Not For Use in Humans. |
| Product Types | ||
| ◆ Bioactive Small Molecules | ||
| BSM-0001 | KW 2449 | Inquiry |
| BSM-0002 | AT9283 | Inquiry |
| BSM-0003 | PHA-680632 | Inquiry |
| BSM-0004 | TAK-901 | Inquiry |
| BSM-0005 | SQ 22536 | Inquiry |
| Related Gene / Proteins | |||
| AUH | Aurka | AurkB | AurkC |
| FAK | FAM171B | FANCA | FANCB |
| FANCC | FANCE | FANCG | FANCI |
| Flt1 | Flt3 | Flt4 | TRA2A |
| TRAF4 | TRAF5 | TRAF6 | TRAK2 More > |
| TRBP | TRDMT1 | TREX1 | TRF2 |
| TRIM11 | TRIM13 | TRIM16 | TRIM17 |
| TRIM2 | TRIM21 | trim24 | TRIM26 |
| TRIM28 | TRIM3 | TRIM33 | TRIM34 |
| TRIM35 | TRIM36 | TRIM37 | TRIM38 |
| TRIM39 | TRIM4 | TRIM5 | TRIM55 |
| TRIM6 | TRIM63 | TRIM66 | TRIM68 |
| TRIM8 | TRIM9 | TRIML1 | TRIP4 |
| Tristetraprolin | TRIT1 | TrkA | TRMT2A |
| TRMT44 | TRMT5 | TRMT6 | TROVE2 |
| TRUB2 | TRX1 | TRβ1 | |
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