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 (1568):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-N3225
    Myricanol 33606-81-4 98.0%
    Myricanol is a diarylheptanoid and a Nampt activator. Myricanol exerts anti-inflammatory effects and alleviates glucocorticoid-induced muscle atrophy by increasing Sirtuin 1 (SIRT1) and PRDX5 activities while regulating inflammatory factors. Myricanol exhibits growth inhibition and induces apoptosis in human lung adenocarcinoma A549 cells. Myricanol promotes autophagy-mediated clearance of microtubule-associated protein tau to exert neuroprotective effects. Myricanol protects cardiovascular function by inhibiting PDGFRβ and NF-κB signaling pathways. Myricanol activates mitochondrial transcription factor A (TFAM) expression to exert anti-renal fibrosis effects. Myricanol improves insulin resistance through AMPK activation.
    Myricanol
  • HY-15599
    SSR128129E 848318-25-2 99.85%
    SSR128129E is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
    SSR128129E
  • HY-114211
    SGC8158
    SGC8158 is an inhibitor of PRMT7 and can be used to study the cellular function of PRMT7. SGC8158 decreases monomethylarginine levels of Hsp70 (the best characterized PRMT7 substrate). SGC8158 induces growth inhibition in various cancer cells (IC50: 2-9 μM), as well as multidrug-resistant (MDR) cancer cells. SGC8158 also enhances Doxorubicin (HY-15142A) induced DNA damage and Its cytotoxicity.
    SGC8158
  • HY-126940
    Furanodiene 19912-61-9 99.83%
    Furanodiene is a natural terpenoid isolated from Rhizoma Curcumae. Furanodiene plays anti-cancer effects through anti-angiogenesis and inducing ROS production, DNA strand breaks and apoptosis. Furanodiene suppresseed efflux transporter Pgp (P-glycoprotein) function and reduced Pgp protein level.
    Furanodiene
  • HY-N10264
    Avrainvillamide 269741-97-1
    Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively.
    Avrainvillamide
  • HY-110208
    BRD9876 32703-82-5 99.37%
    BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research.
    BRD9876
  • HY-10528S
    Tasquinimod-d3 1416701-99-9 99.34%
    Tasquinimod-d3 (ABR-215050-d3) is the deuterium labeled Tasquinimod (HY-10528). Tasquinimod is an oral antiangiogenic agent, which plays an important role in castration-resistant prostate cancer. Tasquinimod binds to the regulatory Zn2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor.
    Tasquinimod-d<sub>3</sub>
  • HY-19753
    KS176 1253452-78-6 99.09%
    KS176 is a selective BCRP inhibitor (IC50 values are 0.59 and 1.39 μM in Pheo A and Hoechst assays, respectively). KS176 can be used in the research of cancer.
    KS176
  • HY-N6015
    Bacopasaponin C 178064-13-6 99.76%
    Bacopasaponin C is an orally active natural glycoside. Bacopasaponin C can be isolated from Bacopa monniera. Bacopasaponin C inhibits Verapamil (HY-14275)-stimulated P-gp ATPase activity with an IC50 of 57.83 μg/mL. Bacopasaponin C has antitumor activity against sarcomas. Bacopasaponin C has antiparasitic activity against Leishmania donovani.
    Bacopasaponin C
  • HY-151606
    Akt3 degrader 1 2836342-69-7
    Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomesOsimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer.
    Akt3 degrader 1
  • HY-163475
    CXCL-CXCR1/2-IN-1 2415653-55-1 99.64%
    CXCL-CXCR1/2-IN-1 is an orally active ELR+CXCL-CXCR1/2 pathway inhibitor with an EC50 of 42.7 nM for CXCR2. CXCL-CXCR1/2-IN-1 shows anticancer and antiangiogenic effects.
    CXCL-CXCR1/2-IN-1
  • HY-108640A
    HLI373 dihydrochloride 1782531-99-0 98.0%
    HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.
    HLI373 dihydrochloride
  • HY-W010649
    Isoxazole 288-14-2 99.98%
    Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor​.
    Isoxazole
  • HY-152188
    AKR1C3-IN-9 2924824-43-9 99.77%
    AKR1C3-IN-9 is a selective inhibitor of Aldo-keto Reductase 1C3 (AKR1C3) with an IC50 value of 8.92 nM. AKR1C3-IN-9 significantly reverses the Doxorubicin (HY-15142A) (DOX) resistance in a resistant breast cancer cell line.
    AKR1C3-IN-9
  • HY-123523
    Enocitabine 55726-47-1 99.32%
    Enocitabine is a nucleoside analog, and is a potent DNA replication inhibitor, and a DNA chain terminator. Enocitabine inhibits the replication of human cytomegalovirus. Enocitabine has antileukemic and antiviral activities.
    Enocitabine
  • HY-118982
    CT-2584 166981-13-1 99.40%
    CT-2584 is a chemotherapeutic compound that reduces the expression of NKEF-B in several tumor cell types and kills tumor cells by inducing the production of ROS in mitochondria, commonly used in cancer research.
    CT-2584
  • HY-164552
    ZNU-IMB-Z15 920915-26-0 99.03%
    ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro.
    ZNU-IMB-Z15
  • HY-N6004
    (Rac)-Shikonin 54952-43-1 98.95%
    (Rac)-Shikonin (Shikonin) possesses anti-tumor activity. (Rac)-Shikonin (Shikonin) circumvents cancer agent resistance by induction of a necroptotic death.
    (Rac)-Shikonin
  • HY-13897
    CNX-2006 1375465-09-0 98.42%
    CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC50 below 20 nM for EGFRT790M.
    CNX-2006
  • HY-N1408
    trans-Trimethoxyresveratrol 22255-22-7 99.35%
    Trans-Trimethoxyresveratrol (trans-trismethoxy Resveratrol; (E)-Resveratrol trimethyl ether; trans-3,5,4'-Trimethoxystilbene) is an orally active natural derivative of Resveratrol (HY-16561). Trans-Trimethoxyresveratrol has an enhanced anticancer profile compared to Resveratrol, exhibiting higher potency than resveratrol, with improved cancer cell proliferation inhibition, induction of cell cycle arrest, decreased metastasis, and increased apoptosis. Trans-Trimethoxyresveratrol causes microtubule disassembling and tubulin depolymerization and exerts anti-angiogenic effects through VEGFR2. Trans-Trimethoxyresveratrol can be used for the studies of anti-angiogenic and anti-cancer (such as non-small cell lung cancer and osteosarcoma).
    trans-Trimethoxyresveratrol