mx-1

Rucaparib (PF-01367338) is a PARP protein inhibitor (PARP-1 Ki=1.4 nM) and hexose hexose-6-phosphate dehydrogenase (H6PD) inhibitor with oral activity. Rucaparib exhibits antitumor activity, with activity against desmoplasia-resistant prostate cancer (CRPC).

Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1 2 (Kis: 1.2 0.85 nM).

Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood-brain barrier permeable microtubule-disrupting agent with potent and broad-spectrum cytotoxic activities and significant anticancer efficacy in human MX-1 breast cancer and various mouse xenograft cancer models.

Rucaparib Phosphate (PF-01367338 phosphate) is an inhibitor of PARP (Ki: 1.4 nM for PARP1) that is used in clinical therapy to sensitize cancer cells to chemotherapy.

Compound X10g (PROTAC Hsp90α degrader 1) is a selective agent targeting Hsp90α for degradation and is utilized in breast cancer research. It demonstrates inhibitory effects on the proliferation of breast cancer cell lines, MDA-MB-231, MDA-MB-468, MCF-7, and MX-1, with respective IC50 values of 51.48 μM, 16.46 μM, 8.93 μM, and 11.95 μM [1].

S-72 acts as a microtubule polymerization inhibitor, effective in cell-free assays at concentrations of 1, 3, and 10 µM. At nanomolar levels (IC50s = 15.64 and 26.32 nM, respectively), it diminishes the viability of both MCF-7 and paclitaxel-resistant MCF-7/T breast cancer cells. Moreover, at 50 nM, S-72 impedes migration, invasion, and wound healing in these cell lines. Additionally, at 100 nM, it arrests the cell cycle at the G2/M phase and induces apoptosis in MCF-7/T cells, while also inhibiting stimulator of interferon genes (STING) activation. In vivo, S-72 dosage at 15 mg/kg per day curtails tumor growth in mouse xenograft models of paclitaxel-resistant breast cancer, specifically MCF-7/T and MX-1/T.

Trabectedin (Ecteinascidin 743) has potent antitumor activity and the potential for soft tissue sarcoma and ovarian cancer research. Trabectedin inhibits cell growth of MX-1, MCF7 and MCF7 DXR cells with IC50 values of 0.1 nM, 1.5 nM and 3.7 nM, respectively.

Rucaparib monocamsylate (Rucaparib Camsylate) is a PARP inhibitor (PARP1,Ki of 1.4 nM). Rucaparib Camsylate also displays binding affinity to eight other PARP domains.

LXY6090 is a HIF-1 inhibitor. LXY6090 inhibited the activity of HIF-1 and downregulated the protein level of HIF-1α in breast cancer cells. LXY6090 showed in vivo anticancer efficacy by decreasing the HIF-1α expression in nude mice bearing MX-1 tumor xeno