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 (1432):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-174826
    EGFR-IN-164
    EGFR-IN-164 (Compound 4) is a selective and covalent allosteric EGFR inhibitor. EGFR-IN-164 significantly inhibits the activity of EGFRL858R/T790M/C797S kinase (IC50: 48.1 nM) and proliferation of of EGFR-mutant cells. EGFR-IN-164 can be used for drug resistance of cancer research.
    EGFR-IN-164
  • HY-161825
    Tubulin polymerization-IN-66
    Tubulin polymerization-IN-66 (Compound 13) inhibits colony formation and tubulin polymerization. Tubulin polymerization-IN-66 induces apoptosis. Tubulin polymerization-IN-66 inhibits cell viability of A549, A2780, SKOV3, HCC827 cells, with IC50s of 0.84, 0.38, 0.31, 0.34 nM respectively. Tubulin polymerization-IN-66 is also active against the Paclitaxel (HY-B0015)-resistant cancer cell line A2780/T and its parental cell line A2780.
    Tubulin polymerization-IN-66
  • HY-N7176R
    Kaempferol 3-O-β-D-glucuronide (Standard) 22688-78-4
    Prosulfocarb (Standard) is the analytical standard of Prosulfocarb. This product is intended for research and analytical applications. Prosulfocarb is a herbicide with a rapidly growing use trend. Prosulfocarb is used in winter cereals to help address the problem of increasing biotic resistance of weeds to certain pesticides. Environmental and food effects of prosulfocarb have been observed, and its transfer pattern from target crops to non-target areas has been studied. The volatility effect of prosulfocarb is an important factor explaining the inefficiency of isolated area contamination and marginal protection against residue spread.
    Kaempferol 3-O-β-D-glucuronide (Standard)
  • HY-A0148
    Halofantrine 69756-53-2
    Halofantrine (SKF-102886 free base) is a highly lipophilic antimalarial active against Chloroquine-resistant strains of Plasmodium falciparum. Halofantrine blocks HERG potassium channels.
    Halofantrine
  • HY-129279
    Andrastin A 174232-42-9
    Andrastin A meroterpenoid compound, is a farnesyltransferase inhibitor. Andrastin A inhibits the efflux of anticancer compounds from multidrug-resistant cancer cells. Andrastin A can be isolated from Penicillium species.
    Andrastin A
  • HY-N7118
    Clindamycin hydrochloride monohydrate 58207-19-5
    Clindamycin hydrochloride monohydrate is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin hydrochloride monohydrate resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin hydrochloride monohydrate decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla).
    Clindamycin hydrochloride monohydrate
  • HY-N4108R
    Hypophyllanthin (Standard) 33676-00-5
    Hypophyllanthin (Standard) is the analytical standard of Hypophyllanthin. This product is intended for research and analytical applications. Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity.
    Hypophyllanthin (Standard)
  • HY-N2334R
    Glycochenodeoxycholic acid (Standard) 640-79-9
    Glycochenodeoxycholic acid (Standard) is the analytical standard of Glycochenodeoxycholic acid. This product is intended for research and analytical applications. Glycochenodeoxycholic acid (Chenodeoxycholylglycine) is a relatively toxic bile salt generated in the liver from chenodeoxycholic acid and glycine. Glycochenodeoxycholic acid inhibits Autophagosome formation and impairs lysosomal function by inhibiting lysosomal proteolysis and increasing lysosomal pH in human normal liver cells, leading to the Apoptosis of human hepatocyte cells. Glycochenodeoxycholic acid induces stemness and chemoresistance via activating STAT3 signaling pathway in hepatocellular carcinoma cells (HCC). Glycochenodeoxycholic acid is promising for research in the field of cholestasis desease, hepatocellular carcinoma and primary sclerosing cholangitis (PSC)[1][2][3][4].
    Glycochenodeoxycholic acid (Standard)
  • HY-N15657
    Geiparvarin 36413-91-9
    Geiparvarin is an anticancer agent and an inhibitor of MAO-B (pIC50 = 6.84 μM). Geiparvarin exerts anti-tumor effects by downregulating COX2 expression and inhibiting angiogenesis. Geiparvarin blocks the cell cycle at the G1 phase and induces apoptosis of cancer cells. Geiparvarin has anti-microtubule activity and destroys the cytoskeleton to exert anti-proliferative effects. Geiparvarin has research significance for lung cancer, leukemia, and breast cancer.
    Geiparvarin
  • HY-168858
    TRK-IN-30
    TRK-IN-30 (Compound C11) is the inhibitor for tropomyosin receptor kinase (TRK) that inhibits TRKA, TRKB and TRKC and drug resistant mutant TRKAG595R with an IC50 of 1.8, 0.98, 3.8, and 54 nM, respectively. TRK-IN-30 inhibits the activation of the downstream PI3K/AKT and MEK/ERK signaling pathways. TRK-IN-30 inhibits the colony formation and cell migration of Km-12, arrests the cell cycle at G0/G1 phase, and induces apoptosis in Km-12.
    TRK-IN-30
  • HY-169509
    Topoisomerase I/II inhibitor 8 355400-87-2
    Topoisomerase I/II Inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of Topoisomerase I/II, capable of inducing DNA damage and PARP-1 activation, which subsequently leads to the activation of RIPK1, RIPK3, and MLKL, ultimately triggering necroptosis. Topoisomerase I/II Inhibitor 8 demonstrates remarkable anticancer activity by effectively targeting the nuclei of cancer cells and inducing cell death through necroptosis, showing great clinical potential in circumventing drug resistance in cancer treatment.
    Topoisomerase I/II inhibitor 8
  • HY-174414
    EGFR/HER2-IN-18
    EGFR/HER2-IN-18 is a stable EGFR/HER2 dual inhibitor with IC50 values of 0.09 and 0.08 μM respectively. EGFR/HER2-IN-18 exhibits broad-spectrum anti-cancer activity. EGFR/HER2-IN-18 induces MCF-7 cells apoptosis and inhibits the cell cycle. EGFR/HER2-IN-18 can be used for the study of breast cancer.
    EGFR/HER2-IN-18
  • HY-B0030R
    D-Cycloserine (Standard) 68-41-7
    D-Cycloserine (Standard) is the analytical standard of D-Cycloserine. This product is intended for research and analytical applications. D-Cycloserine is an antibiotic which targets sequential bacterial cell wall peptidoglycan biosynthesis enzymes. D-Cycloserine is a partial NMDA agonist that can improve cognitive functions. D-Cycloserine can be used for multidrug-resistant tuberculosis research.
    D-Cycloserine (Standard)
  • HY-B0421S2
    Mycophenolic acid-13C17 1202866-92-9
    Mycophenolic acid-13C17 (Mycophenolate-13C17) is the 13C labeled Mycophenolic acid (HY-B0421). Mycophenolic acid is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 μM. Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid is an immunosuppressive agent. Antiangiogenic and antitumor effects.
    Mycophenolic acid-<sup>13</sup>C<sub>17</sub>
  • HY-113703
    PD117588 99734-97-1
    PD117588 is a quinolone antibacterial agent with a broad range of antibacterial activity. PD117588 exhibits excellent activity against a variety of Gram-positive and Gram-negative bacteria from cancer patients, especially against all Gram-positive strains, including methicillin-resistant Staphylococcus aureus, coagulase-negative Staphylococci, and Enterococci. PD117588 is also very effective against most Gram-negative bacilli, although ciprofloxacin shows stronger activity against Pseudomonas aeruginosa. Compared with other quinolone antibiotics, the minimum inhibitory concentration of PD117588 outperforms most of the tested microorganisms, including imipenem and ceftazidime.
    PD117588
  • HY-168711
    P-gp inhibitor 27
    P-gp inhibitor 27 (Compound D2) is an inhibitor for P-glycoprotein (P-gp), that downregulates the expression of P-gp and MRP1, increases the Rh123 accumulation in A2780/T cell, and reverses multidrug resistance to Paclitaxel (HY-B0015) (EC50 is 88 nM) and Cisplatin (HY-17394).
    P-gp inhibitor 27
  • HY-106072
    Vinzolidine 67699-40-5
    Vinzolidine is a semisynthetic derivative of the catharanthus alkaloid. Vinzolidine exerts its cytotoxic effect on tumor cells by interfering with microtubulin polymerization, thereby inhibiting cell division. Vinzolidine can be utilized in research to investigate synergistic effects when combined with other chemotherapeutic agents or biologic therapies, as well as to study cancer cells' tolerance or resistance to these treatments, and to explore approaches to overcome such obstacles.
    Vinzolidine
  • HY-116497
    PH11 1627843-95-1
    PH11 is a novel focal adhesion kinase (FAK) inhibitor that rapidly induces apoptosis in TRAIL-resistant PANC-1 cells when combined with TRAIL, but has no effect on normal human fibroblasts. The study found that PH11 downregulates c-FLIP through inhibition of FAK and phosphatidylinositol-3-kinase (PI3K)/AKT pathways, thereby restoring the TRAIL apoptotic pathway, suggesting that this combination therapy may provide an attractive therapeutic strategy for the safe and effective treatment of pancreatic cancer. PH11 selectively inhibits c-FLIP expression by modulating upstream signaling pathways and may represent an innovative therapeutic strategy. Although further work is needed to fully elucidate the mechanism of PH11-induced TRAIL sensitization, we believe that our results will provide a new approach to target c-FLIP without the risk of interfering with caspase-8 processing, which could potentially lead to TRAIL resistance. This study also suggests a role for the FAK/AKT signaling pathway in regulating c-FLIP expression in TRAIL-induced apoptosis, and this understanding will provide important clues to control the resistance mechanism to optimize the potential of TRAIL-based pancreatic cancer treatment.
    PH11
  • HY-162714
    C3N-Dbn-Trp2 2631659-57-7
    C3N-Dbn-Trp2 is an inhibitor for ATP-binding cassette transporter ABCB1. C3N-Dbn-Trp2 inhibits the ABCB1-mediated Rhodamine 123 (HY-D0816) efflux in cells HEK293T and HCT-15 with IC50 of 5.9 µM and 2.2 µM. C3N-Dbn-Trp2 inhibits the Doxorubicin (HY-15142A) efflux, enhances the cytotoxicity of Doxorubicin in ABCB1-expressing cells.
    C3N-Dbn-Trp2
  • HY-N3981
    Guajadial 959860-49-2
    Guajadial, a caryophyllene-based meroterpenoid, has anti-estrogenic and anticancer effect. Guajadial reverses multidrug resistance in cancer. Guajadial can be isolated from Psidium guajava leaves.
    Guajadial