COTI-2 (COTI2) is an orally available thiosemicarbazone that may act on mutant forms of p53 and PI3K/AKT/mTOR pathway; induces apoptosis in a wide variety of human tumor cells in culture (IC50s<40 nM), inhibits the proliferation of colorectal cancer cell lines more effectively than cetuximab and erlotinib; shows superior activity against tumor, and is safe and well-tolerated in vivo.
Phase 1 Clinical
PTC-596 (PTC596) is a novel, orally active, small molecule inhibitor of BMI-1 that accelerates BMI-1 degradation, inhibits AML cells growth with IC50 of <100 nM; PTC-596 is a direct microtubule polymerization inhibitor; reduces total BMI-1 protein levels by 87% and 61% in MOLM-13 and OCI-AML3 cells at 100 nM, induces apoptosis and reduces the levels of ubiquitylated histone H2A; downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia progenitor cells.
Pamiparib (BGB-290, BGB290) is a highly potent, selective and brain penetrant PARP1/2 inhibitor with potent anti-tumor activity.
Phase 2 Clinical
Cridanimod (10-carboxymethyl-9-acridanone, 10-CMA, XBIO-101) is a potent type I interferon (IFN) inducer that directly binds to STING and triggers a strong antiviral response through the TBK1/IRF3 route; displays extraordinary activity in phosphorylating IRF3 in the murine system; also increases progesterone receptor (PrR) expression in endometrial tissue.
Triapine (3-AP, PAN-811, OCX191, NSC 663249) is a potent ribonucleotide reductase inhibitor with broad spectrum antitumor activity.
Trabectedin (Ecteinascidin-743, ET-743, Ecteinascidin) is a marine alkaloid isolated from the Caribbean tunicate Ecteinascidia turbinata that shows remarkably anticancer activity in a variety of in vitro and in vivo systems; a DNA minor groove, guanine-specific alkylating agent; shows hign potency against ovarian carcinoma xenografts.
MK-4827 (Niraparib, MK4827) is a highly potent PARP inhibitor with IC50 of 3.8 nM/2.1 nM for PARP1/PARP2; inhibits PARP activity with EC50=4 nM in a whole cell assay, and inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10−100 nM range; well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer.
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