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-W705354
    Vismodegib-d4 1450990-33-6
    Vismodegib-d4 is deuterium labeled Vismodegib. Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively.
    Vismodegib-d<sub>4</sub>
  • HY-N2651
    5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone 1268140-15-3
    5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone (compound 1), a flavonoid, is a potent ABCG2 inhibitor with an IC50 of 6.6 μM.
    5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone
  • HY-17367R
    Atazanavir (Standard) 198904-31-3
    Atazanavir (Standard) is the analytical standard of Atazanavir. This product is intended for research and analytical applications. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.
    Atazanavir (Standard)
  • HY-50880R
    Elacridar hydrochloride (Standard) 143851-98-3
    Elacridar (hydrochloride) (Standard) is the analytical standard of Elacridar (hydrochloride). This product is intended for research and analytical applications. Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer.
    Elacridar hydrochloride (Standard)
  • HY-101621
    Teludipine hydrochloride 108700-03-4
    Teludipine is a lipophilic calcium channel blocker.
    Teludipine hydrochloride
  • HY-13760
    Tasidotin hydrochloride 623174-20-9
    Tasidotin hydrochloride is a peptide analog of the antimitotic depsipeptide dolastatin 15, as an inhibitor of microtubule assembly and microtubule dynamics.
    Tasidotin hydrochloride
  • HY-133838
    Ilmofosine 83519-04-4
    Ilmofosine (BM41440) is a potent and selective protein kinase C inhibitor. Ilmofosine induces cell cycle arrest at the G2 phase. Ilmofosine also is an anti-leishmanial agent.
    Ilmofosine
  • HY-171183
    AB8939 1974336-09-8
    AB8939 is an effective small moleculeMicrotubule/Tubulin polymerization inhibitor with anti-tumor activity (it inhibits tumor cell proliferation with an IC50 of less than 10 nM). AB8939 can effectively evade resistance mechanisms mediated by things like P-glycoprotein and myeloperoxidase. AB8939 can induce G2/M phase cell cycle arrest and apoptosis in cells.
    AB8939
  • HY-N0716
    Berberine 2086-83-1
    Berberine (Natural Yellow 18) is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine (Natural Yellow 18) induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine (Natural Yellow 18) has antineoplastic properties. The sulfate form (HY-N0716B) improves bioavailability.
    Berberine
  • HY-N13157
    11α-O-Benzoyl-12β-O-acetyltenacigenin B 154022-52-3
    11α-O-Benzoyl-12β-O-acetyltenacigenin B is a P-glycoprotein (Pgp) inhibitor derived from Marsdenia tenacissima and belongs to the Tenacigenin B (HY-N1168) derivatives. 11α-O-Benzoyl-12β-O-acetyltenacigenin B can inhibit multidrug resistance (MDR) caused by P-glycoprotein (Pgp) overexpression in HepG2/Dox cells and holds potential for research in the field of cancer.
    11α-O-Benzoyl-12β-O-acetyltenacigenin B
  • HY-N14144
    Cremimycin 182285-29-6
    Cremimycin has anti-Gram-positive bacteria activity including methicillin-resistant Staphylococcus aureus (MRSA), MIC is 0.2-0.39 μg/mL. Cremimycin shows cytotoxicity to mouse tumor cell lines P388, L1210, IMC, S180, B16 and SS3 in vitro.
    Cremimycin
  • HY-N0402R
    Artemether (Standard) 71963-77-4
    Artemether (Standard) is the analytical standard of Artemether. This product is intended for research and analytical applications. Artemether is an anti-malarial compound that targets drug-resistant strains of falciparum malaria.
    Artemether (Standard)
  • HY-113759
    Saquayamycin A 99260-65-8
    Saquayamycin A has antimicrobial effect, but it has weaker effect against Gram-negative bacteria. Saquayamycin A has inhibitory effect on leukemia P388 cells and Adriamycin-resistant P388 cells.
    Saquayamycin A
  • HY-168649
    JH-LPH-107 3053068-92-8
    JH-LPH-107 is a LpxH inhibitor. JH-LPH-107 exhibits a low rate of spontaneous resistance and a high safety window in vitro..
    JH-LPH-107
  • HY-164393
    ON044580 1035199-04-2
    ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling.
    ON044580
  • HY-101561R
    Avapritinib (Standard) 1703793-34-3
    Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2.
    Avapritinib (Standard)
  • HY-13646AR
    Encequidar mesylate (Standard) 849675-87-2
    Encequidar (mesylate) (Standard) is the analytical standard of Encequidar (mesylate). This product is intended for research and analytical applications. Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.
    Encequidar mesylate (Standard)
  • HY-129037
    BCRP-IN-1 765899-28-3
    BCRP-IN-1 (compound 48) is a potent inhibitor of breast cancer resistance protein (BCRP), with IC50s of 2.92 μM and 2.46 μM in Hoechst 33342 assay and Pheophorbide A assay, respectively.
    BCRP-IN-1
  • HY-N7305
    Jatrophane 5 210108-89-7
    Jatrophane 5 is a natural product of Jatropha carcas L. Jatrophane 5 has powerful inhibition of P-gp, higher than R(+)-verapamil (HY-14275) and Tariquidar (HY-10550) in colorectal multi-drug resistant cells (DLD1-TxR).
    Jatrophane 5
  • HY-126802
    Saquayamycin B1 99260-68-1
    Saquayamycin B1 has antimicrobial effect, but it has weaker effect against Gram-negative bacteria. Saquayamycin B1 has inhibitory effect on leukemia P388 cells and Adriamycin-resistant P388 cells.
    Saquayamycin B1