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 (1438):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-111061
    GTX-758 938067-78-8 99.59%
    GTX-758 is an orally active, nonsteroidal, selective agonist of ERα. GTX-758 plays an important role in castration resistant prostate cancer (CRPC) research.
    GTX-758
  • HY-B1381A
    Cefixime trihydrate 125110-14-7 99.77%
    Cefixime trihydrate (FR-17027 trihydrate) is an antibiotic and a third generation cephalosporin antibiotic, useful for the treatment of a number of bacterial infections.
    Cefixime trihydrate
  • HY-116871
    YKL-1-116 1957202-71-9 98.67%
    YKL-1-116 is a selective and covalent inhibitor of Cdk7. YKL-1-116 does not target Cdk9, Cdk12, or Cdk13. YKL-1-116 is more potent than THZ1 (HY-80013) toward both Cdk7WT and Cdk7as, although Cdk7as is relatively resistant to this compound as well.
    YKL-1-116
  • HY-N1423S1
    Glycocholic acid-d5 2170091-95-7
    Glycocholic acid-d5 is the deuterium labeled Glycocholic acid. Glycocholic acid is a bile acid with anticancer activity, targeting against pump resistance-related and non-pump resistance-related pathways.
    Glycocholic acid-d<sub>5</sub>
  • HY-117161
    ZINC05626394 189057-68-9 99.8%
    ZINC05626394 is a cytochrome b5 reductase 3 inhibitor with activity by increasing nitric oxide bioavailability. ZINC05626394 may have potential applications in anti-cancer suppression, especially in combination with antibody drug conjugates (ADCs) and immune checkpoint inhibitors. The efficacy of ZINC05626394 may be limited by different mechanisms, including antigen-related resistance and failure of endocytosis.
    ZINC05626394
  • HY-148366
    NecroIr2 98.99%
    NecroIr2 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr2 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr2 activates receptor-interacting serine-threonine kinase 3 (RIPK3) and mixed lineage kinase domain-like pseudokinase (MLKL), and regulates CDK4 expression.
    NecroIr2
  • HY-113636
    Kazinol A 99624-28-9
    Kazinol A induces cytotoxic effects in human bladder cancer cells, including the cisplatin-resistant T24R2.
    Kazinol A
  • HY-118899
    XR5944 343247-32-5
    XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer.
    XR5944
  • HY-124663
    CBK289001 1212663-24-5 99.74%
    CBK289001 is a tartrate-resistant acid phosphatase (TRAP/ACP5) inhibitor. CBK289001 inhibits TRAP 5bMV, TRAP 5bOX and TRAP 5aOX with IC50s of 125 µM, 4.21 µM and 14.2 µM, respectively.
    CBK289001
  • HY-156753
    NorA-IN-1 1389310-69-3
    NorA-IN-1 (Compound 16) is a NorA inhibitor. NorA-IN-1 inhibits NorA efflux pump in everted membrane vesicles. NorA-IN-1 can be used for research of multidrug resistance.
    NorA-IN-1
  • HY-173162
    GPV0057 86383-89-3 99.20%
    GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel Kir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of Kir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, Kir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome.
    GPV0057
  • HY-114982
    KEA1-97 2138882-71-8 98.05%
    KEA1-97 is a selective Thioredoxin-caspase 3 interaction disruptor (IC50=10 μM). KEA1-97 disrupts the interaction of thioredoxin with caspase 3, activates caspases, and induces apoptosis without affecting thioredoxin activity.
    KEA1-97
  • HY-146393
    PROTAC CYP1B1 degrader-1 2411389-67-6 98.09%
    PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer.
    PROTAC CYP1B1 degrader-1
  • HY-157169
    IBL-302 1414455-21-2 98.21%
    IBL-302 (AMU302) is an orally available dual-signaling inhibitor of PIM and PI3K/AKT/mTOR with activity against breast cancer and neuroblastoma. IBL-302 demonstrated in vivo efficacy in a nude mouse xenograft model, inhibiting trastuzumab (HY-P9907) resistance challenges. IBL-302 also enhances the effects of common cytotoxic chemotherapy drugs cisplatin (HY-17394), doxorubicin (HY-15142A), and etoposide (HY-13629).
    IBL-302
  • HY-116852
    Thiocolchicine 2730-71-4 99.77%
    Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 µM) and competitively binds to tubulin with a Ki of 0.7 µM. Thiocolchicine induces cell apoptosis. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.
    Thiocolchicine
  • HY-N2598
    Methyl oleate 112-62-9 ≥98.0%
    Methyl oleate is a fatty acid methyl ester (FAME) with anti-extended spectrum β-Lactamase (ESBL) potential, anticancer and antibacterial activities. Methyl oleate substantially improves the antioxidation ability but markedly impaired the antiwear capacity of zinc dialkyldithiophosphate (ZDDP). Methyl oleate is promising for research of ESBL producing multi drug resistant (MDR) pathogens.
    Methyl oleate
  • HY-123159
    AKI603 1432515-73-5 98.03%
    AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells.
    AKI603
  • HY-138072
    EMI1 35773-42-3 99.78%
    EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC).
    EMI1
  • HY-131468
    Picoplatin 181630-15-9 98.5%
    Picoplatin (AMD473) is a platinum-based antineoplastic agent. Picoplatin is specifically to circumvent thiol-mediated drug resistance by sterically hindering its reaction with glutathione (GSH) while still retaining the ability to form cytotoxic lesions with DNA.
    Picoplatin
  • HY-155993
    YCH1899 3032451-66-1 99.39%
    YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats.
    YCH1899