Antitumoral Phortress Small Molecule (Tool Compound)
Cat. #:
151839
Sub-type:
Antitumoral
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Active against breast, ovarian and renal carcinomas. Taken up into sensitive cells followed by aryl hydrocarbon receptor binding and translocation into the nucleus. Requires metabolic activation by cytochrome P450 to generate cytotoxic species. Induces expression of CYP1A1 and generates adducts in the DNA of sensitive MCF7 and IGROV-1 cells.
Antitumoral Quinol2 Small Molecule (Tool Compound)
Cat. #:
151840
Sub-type:
Inhibitor
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Displays in vivo antitumor activity against human RXF 944XL renal xenografts in nude NMRI mice. Inhibits thioredoxin reductase with potencies correlated with their antiproliferative and cytotoxic efficacies. Potent activity against renal, colon, and breast cancer cell lines in the NCI 60-cell panel. Shows potent antitumor activity in HCT 116 and HT 29 human colon as well as MCF 7 and MDA 468 human breast cancer cell lines.
Mps1 inhibitor CCT251455 Small Molecule (Tool Compound)
Cat. #:
152625
Sub-type:
Inhibitor
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Application:
CCT251455 displays a favorable oral pharmacokinetic profile, shows dose-dependent inhibition of MPS1 in an HCT116 human tumor xenograft model, and is an attractive tool compound to elucidate further the therapeutic potential of MPS1 inhibition. In Female Balb/C mice it had an oral bioavailabilty of 83%.
Dual DNA-PK/PI3K inhibitor KU-0060648 Small Molecule (Tool Compound)
Cat. #:
152709
Sub-type:
Inhibitor
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Application:
KU-0060648 enhances the anti-tumour activity of etoposide in both MCF7 and SW620 xenograft models, and has single-agent activity in the MCF7 xenograft model. KU-0060648 exhibits differential effects on growth inhibition, but is not profoundly cytotoxic in a panel of human cancer cell lines. It inhibits DNA-PK and PI-3K with greater potency in MCF7 than SW620 cell using cell-based assays. Five-day exposure to 1 mM KU-0060648 inhibits cell proliferation by more than 95% in MCF7 cells but only b…
CDK2 inhibitor NU6301 Small Molecule (Tool Compound)
Cat. #:
152754
Sub-type:
Inhibitor
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The prodrug NU6301 rapidly generated NU6102 in vitro in mouse plasma, and tumour NU6102 levels in vivo consistent with activity in vitro. Eight or 12 hourly dosing of 120 mg/kg NU6301 for 10 days was well tolerated in SKUT-1B tumour-bearing mice and inhibited Rb phosphorylation in tumour tissue. Two (8 hourly dosing) and 3 (12 hourly dosing) day tumour growth delay was observed (p=0.04 and p=0.007, respectively) following NU6301 administration. NU6102 selectively inhibited the growth of CDK2 WT (wild type) versus KO MEFs (knockout mouse embryo fibroblasts) (GIâ â (concentration required to inhibit cell growth by 50%) 14 ÎźM versus >30 ÎźM), and was more growth-inhibitory in p53 mutant or null versus p53 WT cells (p=0.02), and in Rb (retinoblastoma protein) WT SKUT-1B versus SKUT 1 Rb deficient cells (p=0.01). In SKUT-1B cells NU6102 induced a G2 arrest, inhibition of Rb phosphorylation and cytotoxicity (LCâ â 2.6 ÎźM for a 24h exposure).
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