2. Cancer
  3. Cancer Drug Resistance

Cancer Drug Resistance

Drug resistance in chemotherapy, radiotherapy, molecular targeted therapy and immunotherapy is one of the main causes of death due to cancer. Gene mutations, non-genetic and epigenetic mechanisms to evade drug actions can promote the occurrence of drug resistance and treatment failure. Simultaneous resistance to multiple drugs with different chemical structures, different mechanisms of action and different targets is known as multidrug resistance (MDR). MDR can be related to a variety of mechanisms, including overexpression of drug efflux pumps(ABC transporter family), decreased drug uptake, mutation/loss of receptors, altered apoptotic pathway, enhanced DNA repair and drug metabolism(glutathione S-transferase, CYP450).

ABC transporters are membrane protein superfamily that can mediate MDR mechanism in many types of cancer. Some members of this superfamily includes MDR-associated protein-1(MRP1/ABCC1), breast cancer resistant proteins(ABCG2/BRCP) and P-glycoprotein(P-gp/ABCB1/MDR1). Among them, P-gp is the most extensively characterized efflux pump of MDR, and plays an important role in many cancers such as breast cancer, human lung cancer, ovarian cancer, and colorectal cancer.

The design of antitumor drugs that are able to evade or reverse MDR is rapidly evolving in the anti-cancer drug discovery field. Nanoparticle-based drug delivery platforms have been widely studied in cancer treatment, and become optimal carriers to reverse the limitations encountered in the use of traditional drug formulations, by influencing/manipulating ABC transporter-associated drug efflux mechanisms.

Cancer Drug Resistance Related Products (1368):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-117452
    LY-402913 334970-65-9 99.86%
    LY-402913 is a selective multidrug resistance protein (MRP1) inhibitor.
    LY-402913
  • HY-13538A
    Gemcitabine elaidate hydrochloride 2918768-08-6 99.89%
    Gemcitabine elaidate (CP-4126) hydrochloride is lipophilic pro-agent of Gemcitabine. Gemcitabine elaidate hydrochloride is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate hydrochloride exhibits anti-tumor activity.
    Gemcitabine elaidate hydrochloride
  • HY-W009538
    5'-Deoxy-5-fluorocytidine 66335-38-4 99.91%
    5'-Deoxy-5-fluorocytidine (5-Fluoro-5'-deoxycytidine) is a cytidine analog and metabolite of Capecitabine (HY-B0016). 5'-Deoxy-5-fluorocytidine is converted from Capecitabine by carboxylesterase in the liver. 5'-Deoxy-5-fluorocytidine is deaminated by cytidine deaminase to generate 5'-deoxy-5-fluorouridine, which is finally converted into 5-fluorouracil (HY-90006) by thymidine phosphorylase in tumor tissues to exert anti-tumor effects. 5'-Deoxy-5-fluorocytidine is used in the researches for solid tumors such as colorectal cancer, non-small cell lung cancer and breast cancer.
    5'-Deoxy-5-fluorocytidine
  • HY-N4288
    4-Methylesculetin 529-84-0 98.09%
    4-Methylesculetin is an orally active coumarin derivative, with potent anti-oxidant and anti-inflammatory activities. 4-Methylesculetin inhibits myeloperoxidase activity. 4-Methylesculetin protects bone resorption by reducing the elevated levels of bone-joint exoglycosidases, cathepsin-D and tartrate resistant acid phosphatases. 4-Methylesculetin ameliorats the upregulated non-enzymatic inflammatory markers like TNF-α, IL-1β, IL-6, COX-2 and PGE2, which is promising for research of inflammatory diseases.
    4-Methylesculetin
  • HY-100555
    CH5138303 959763-06-5 99.05%
    CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model.
    CH5138303
  • HY-N0007A
    Bisdemethoxycucurmin 24939-16-0 98.96%
    Bisdemethoxycucurmin (Curcumin III) is a curcuminoid compound and an inhibitor of P-glycoprotein and ferroptosis. Bisdemethoxycucurmin exhibits multiple activities such as anti-oxidation, anti-inflammation and anti-tumor. Bisdemethoxycucurmin can be used for the research of tumors and inflammatory diseases.
    Bisdemethoxycucurmin
  • HY-N8321
    5-O-Caffeoylshikimic acid 73263-62-4 99.28%
    5-O-Caffeoylshikimic acid can be used in the study for NSCLC.
    5-O-Caffeoylshikimic acid
  • HY-13574A
    Biricodar 159997-94-1 99.31%
    Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
    Biricodar
  • HY-10207
    Dovitinib lactate 692737-80-7 99.75%
    Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
    Dovitinib lactate
  • HY-14672
    Soblidotin 149606-27-9 99.29%
    Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10 derivative and inhibitor of tubulin polymerization.
    Soblidotin
  • HY-114315
    NQO1 substrate 2304503-05-5 98.02%
    NQO1 substrate acts as an efficient NQO1 substrate and may be a new option for the treatment of NQO1-overexpresssing drug-resistant NSCLC.
    NQO1 substrate
  • HY-B0965A
    Thioridazine 50-52-2 99.50%
    Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
    Thioridazine
  • HY-163198
    ASCT2-IN-1 3032651-18-3 98.21%
    ASCT2-IN-1 (compound 20k) is an ASCT2 inhibitor with IC50 values of 5.6 μM and 3.5 μM in cells A549 and HEK293, respectively. ASCT2-IN-1 induces cell apoptosis. ASCT2-IN-1 inhibits tumor growth.
    ASCT2-IN-1
  • HY-128914
    Tubulysin 1943604-24-7 99.53%
    The Tubulysin family of secondary metabolites was originally isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. These compounds are potent microtubule destabilizers and anti-microtubule toxins (anti-microtubule toxins), with effective IC50 concentrations against multidrug-resistant cancer cell lines. In the picomole range. Tubulysins are ideal candidates for incorporation into small active molecule conjugate (SMDC) delivery systems and are commonly used in ADC synthesis as ADC cytotoxins (ADC Cytotoxin).
    Tubulysin
  • HY-14821
    Namitecan 372105-27-6 99.25%
    Namitecan is a potent topoisomerase I inhibitor, with antitumor property.
    Namitecan
  • HY-137449
    Rintodestrant 2088518-51-6 99.91%
    Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor.
    Rintodestrant
  • HY-151517
    SOS1-IN-14 2793405-20-4 99.60%
    SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-14 has better potent tumor suppression than BI-3406 (HY-125817).
    SOS1-IN-14
  • HY-125486
    Reversin 121 174630-04-7 99.31%
    Reversin 121 is a P-glycoprotein inhibitor. Reversin 121 increases the ATPase activity of MDR1. Reversin 121 reverses P-glycoprotein-mediated multidrug resistance. Reversin 121 can be used in the research of cancers.
    Reversin 121
  • HY-B0609
    Fosfomycin tromethamine 78964-85-9 99.69%
    Fosfomycin (MK-0955) tromethamine is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin tromethamine shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
    Fosfomycin tromethamine
  • HY-111678
    ML230 1776055-05-0 99.65%
    ML230 (CID44640177; SID 88095709) is a selective inhibitor of ATP-binding cassette (ABC) transporter ABCG2, and 36-fold selective for ABCG2 over ABCB1 with EC50s values of 0.13 μM and 4.65 μM, respectively.
    ML230