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-19341
    Compound 401 168425-64-7 99.97%
    Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM) that also targets mTOR but not PI3K in vitro.
    Compound 401
  • HY-145931
    CC214-2 1228012-18-7 98.41%
    CC214-2 is an oral active and selective mTOR kinase inhibitor. CC214-2 targets to both of mTORC1 (pS6) and mTORC2 (pAktS473). CC214-2 induces autophagy, which is a potential target for host-directed therapy (HDT) in tuberculosis. CC214-2 exhibits synergistic bactericidal and sterilizing activity agasinst tuberculosis (TB), and shortens the treatment duration. CC214-2 also inhibits Rapamycin (HY-10219)-resistant signaling and the growth of glioblastomas in vitro and in vivo.
    CC214-2
  • HY-N1243
    Tubulysin B 205304-87-6 99.88%
    Tubulysin B is a highly cytotoxic peptide and potent microtubule destabilizing agents isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin B has IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties.Tubulysin B is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
    Tubulysin B
  • HY-P1823
    C-Reactive Protein (CRP) (174-185) 147516-85-6 99.88%
    C-Reactive Protein (CRP) is an anti-pneumococcal plasma protein that can serve as an inflammatory marker. C-Reactive protein can protect mice from pneumococcal infection by activating complement. C-Reactive protein can inhibit the activation of caspase-3/9 through the CD64/AKT/mTOR pathway, thereby promoting chemotherapy resistance in mice with tongue squamous cell carcinoma.
    C-Reactive Protein (CRP) (174-185)
  • HY-13053
    Depulfavirine 867365-76-2 99.48%
    RO-0335 is a novel and potent diphenylether nonnucleoside reverse transcriptase inhibitor(NNRTI). RO-0335 inhibits Wt HIV-1 with an IC50 of 1.1 nM and retained activity (IC50< 100 nM) against 92% of a large number of NNRTI-resistant clinical isolates.
    Depulfavirine
  • HY-P5581
    Alloferon 1 347884-61-1 99.97%
    Alloferon 1 is an antiviral and antitumoral peptide. Alloferon 1 stimulates natural cytotoxicity of human peripheral blood lymphocytes. Alloferon 1 also induces IFN synthesis, and enhances antiviral and antitumor resistance in mice. Alloferon 1 also shows anti-inflammatory activity in λ-carrageenan-induced paw edema model. Alloferon 1 can be isolated from the blood of the blow fly Calliphora vicina (Diptera).
    Alloferon 1
  • HY-N7591
    Millepachine 1393922-01-4 99.55%
    Millepachine is a bioactive natural chalcone from Chinese herbal medicine Millettia pachycarpa Benth, exhibits strong antitumor effects against numerous human cancer cells both in vitro and in vivo.
    Millepachine
  • 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-158118
    Lys(CO-C3-p-I-Ph)-OMe 2088426-96-2
    Lys(CO-C3-p-I-Ph)-OMe is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules (such as Ac-PSMA-trillium). Lys(CO-C3-p-I-Ph)-OMe can increase the residence time of Ac-PSMA-trillium in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-OMe also reduces salivary gland absorption of Ac-PSMA-trillium, potentially extending its half-life. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC).
    Lys(CO-C3-p-I-Ph)-OMe
  • HY-19753
    KS176 1253452-78-6 99.09%
    KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.
    KS176
  • 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-110201
    Estrogen receptor modulator 1 63676-22-2 99.91%
    Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.
    Estrogen receptor modulator 1
  • 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-118982
    CT-2584 166981-13-1
    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-10844S
    Pretomanid-d4 1346617-34-2 99.39%
    Pretomanid-d4 is the deuterium labeled Pretomanid. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
    Pretomanid-d<sub>4</sub>
  • HY-15456
    NVP-BVU972 1185763-69-2 98.78%
    NVP-BVU972 is an selective and potent Met inhibitor, with an IC50 of 14 nM. NVP-BVU972 also exhibits good anti-proliferative activity against Met with drug-resistant mutations and inhibits phosphorylation. NVP-BVU972 can be used in study of cancer.
    NVP-BVU972
  • 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-N1423R
    Glycocholic acid (Standard) 475-31-0
    Glycocholic acid (Standard) is the analytical standard of Glycocholic acid. This product is intended for research and analytical applications. Glycocholic acid is a bile acid with anticancer activity, targeting against pump resistance-related and non-pump resistance-related pathways.
    Glycocholic acid (Standard)
  • HY-12965
    S49076 1265965-22-7 99.44%
    S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
    S49076
  • HY-111414
    Hsp90-Cdc37-IN-1 2227303-22-0 99.66%
    Hsp90-Cdc37-IN-1 is an Hsp90-Cdc37 interaction disruptor that inhibit cell migration and reverse agent resistance, with an IC50 of 140 nM.
    Hsp90-Cdc37-IN-1