GPX4-IN-6 (Compound C25) is a GPX4 covalent inhibitor with an IC50 value of 0.13 μM. GPX4-IN-6 (Compound C25) can induce ferroptosis for the research of triple-negative breast cancer (TNBC) [1].
ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3.
10NH2-11F-Camptothecin is an antibody drug conjugates (ADC). 10NH2-11F-Camptothecin has anti-tumor activity. 10NH2-11F-Camptothecin can be used for cancer research[1].
Mal-C2-NHS ester is a noncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
MDH1-IN-2 (Compound 7c) is a potent and selelctive inhibitor of MDH1 with an IC50 of 2.27 μM. MDH1-IN-2 has the potential for the research of cancer diseases[1].
Ramucirumab is a human VEGFR-2 antagonist for the treatment of solid tumors[1]. Ramucirumab is a recombinant human immunoglobulin G1 monoclonal antibody that binds to the extracellular binding domain of VEGFR-2 and prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D[2].
Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC50 value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity[1].
8-Allylthioguanosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFRL858R, EGFRExon 19 deletion and EGFRT790M.
PROTAC Linker 22 is a PROTAC linker, which refers to the alkyl chain composition. PROTAC Linker 22 can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
FAK-IN-10 is an inhibitor of FAK with an IC50 of 76.3 μM. FAK-IN-10 exhibits antitumor activity against MCF-7 and A431 cell lines with IC50s of 4.23 and 0.78 μM,respectively[1].
GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
Nedaplatin is a derivative of cisplatin and DNA damage agent.Target: OthersNedaplatin(NDP) is a derivative of cisplatin which produced less nausea & vomiting and nephrotoxicity. the effect of NDP on the 7-ethyl-1-hydroxy-CPT (the active form of CPT-11)-induced inhibitory effect on DNA topoisomerase I was examined. The topoisomerase I-inhibitory effect of 7-ethyl-1-hydroxy-CPT was enhanced 10-fold in the presence of NDP at microgram/milliliter concentrations [1]. NDP was developed as a second generation platinum complex. Because it has greater antitumour activity and lower nephrotoxicity than cisplatin (CDDP). At the high-dose of NDP in FN therapy, a reduction of tumour size and long-term tumour-free survival were frequently observed. The survival effect of the combinations of NDP with 5-FU was superior to those of the combination of CDDP with 5-FU. In conclusion, the sequence-dependent antitumour efficacy and toxicity of the combination of NDP or CDDP with 5-FU was demonstrated in this study, and FN therapy appeared to be the most efficient regimen as a clinical therapy [2].
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice[1].
Vincristine (Leurocristine) is a microtubule-destabilizing agent (MDA). Vincristine (Leurocristine) binds to tubulin and inhibits the formation of microtubules, thereby inhibiting mitosis of the cancer cell. Vincristine (Leurocristine) is used to treat hematologic cancers, such as leukemia and lymphoma, and childhood sarcomas[1][2].
Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor)[1][2].
Avasimibe is an oral inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT) with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively.
Mirvetuximab soravtansine (IMGN853) is an antibody drug-conjugate (ADC) consisting of the cytotoxic maytansinoid, DM4, covalently linked to the humanized monoclonal antibody M9346A. Mirvetuximab soravtansine selectively binds to folate receptor 1 (FOLR1). Mirvetuximab soravtansine has an anti-proliferative effect via growth arrest and augmented DNA damage[1].
6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug.
SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM.
Melatonin D5 is deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Antioxidative and anti-inflammatory properties[1][2][3]. Melatonin is a selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation[4].
Quazomotide is a WT1 class II peptide epitope with sequences of RSDELVRHHNMHQRNMTKL. Quazomotide stimulates a peptide-specific CD4(+) response, to recognize WT1(+) tumor cells. Quazomotide is an immunological agent for active immunization, as well as an antineoplastic agent[1][2].
IA1-8H2 is a non-covalent, non-competitive inhibitor of PHPT1 (IC50: 3.4 μM). IA1-8H2 can be used for research of lung cancer, hepatocarcinoma, and renal cancer[1].
p53 and MDM2 proteins-interaction-inhibitor (racemic) (Compound 2j) is an inhibitor of the interaction between p53 and MDM2 proteins.
Onvatilimab (JNJ-61610588) is a human IgG1κ anti-VISTA (V-domain Ig Suppressor of T-cell Activation) monoclonal antibody. Onvatilimab has an anti-tumor activity[1].
SU11274 is a selective Met inhibitor with IC50 of 10 nM, but has no effects on PGDFRβ, EGFR or Tie2.
Androgen receptor antagonist 7 is an effective androgen receptor (AR) antagonist with an IC50 value of 1.18 µM. Androgen receptor antagonist 7 has biological activity in vitro and inhibits the expression of AR target in a time and dose dependent manner with an GI50 value of 7.9 µM [1].
Fluorobexarotene (compound 20) is a potent retinoid-X-receptor (RXR) agonist, with a Ki value of 12 nM and an EC50 value of 43 nM for RXRα receptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene[1].
A potent, highly selective α4β1 integrin antagonist with Kd of <10 pM; the rate of BIO7662 binding is dependent on the metal ion concentration; directly competes with VCAM-1, CS-1, and BIO1211 for binding to the integrin.
Rostratin B, a cytotoxic disulfide, shows in vitro cytotoxicity against human colon carcinoma (HCT-116) with IC50 of 1.9 μg/mL[1].