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 関連製品 (1943):

製品番号 製品名 CAS 番号 純度 構造式
  • HY-16558
    Butein 487-52-5 99.64%
    Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
    Butein
  • HY-N2515
    Ginsenoside Rk1 494753-69-4 99.90%
    Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures. Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB. Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis. Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway.
    Ginsenoside Rk1
  • HY-15777A
    Ribociclib hydrochloride 1211443-80-9 99.95%
    RRibociclib (LEE011) hydrochloride is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
    Ribociclib hydrochloride
  • HY-B0532A
    Trifluoperazine dihydrochloride 440-17-5 99.98%
    Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.
    Trifluoperazine dihydrochloride
  • HY-18972
    Plixorafenib 1393466-87-9 99.80%
    PLX8394 is a potent and selective BRaf inhibitor, with an IC50 of appr 5 nM for BRAFV600E.
    Plixorafenib
  • HY-17367
    Atazanavir 198904-31-3 99.23%
    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
  • HY-15777B
    Ribociclib succinate 1374639-75-4 99.93%
    RRibociclib (LEE011) succinate is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
    Ribociclib succinate
  • HY-N2143
    Fumitremorgin C 118974-02-0 99.92%
    Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor.
    Fumitremorgin C
  • HY-12037A
    Rigosertib 592542-59-1 99.01%
    Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM.
    Rigosertib
  • HY-162318
    MYC degrader 1 2946670-96-6 99.61%
    MYC degrader 1 (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 restores pRB1 protein activity and re-establishes sensitivity of MYC overexpressing cancer cells to CDK4/6 inhibitors.
    MYC degrader 1
  • HY-17384
    Valspodar 121584-18-7 99.27%
    Valspodar (PSC 833) is a selective P-glycoprotein inhibitor that has been used as an experimental cancer treatment and chemosensitizer.
    Valspodar
  • HY-50880
    Elacridar hydrochloride 143851-98-3 99.93%
    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
  • HY-18630A
    Ro 48-8071 189197-69-1 99.89%
    Ro 48-8071 is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM.
    Ro 48-8071
  • HY-10339
    KW-2449 1000669-72-6 99.91%
    KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABLT315I and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, respectively.
    KW-2449
  • HY-131003
    Taletrectinib 1505515-69-4 99.63%
    Taletrectinib (DS-6051b) is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
    Taletrectinib
  • HY-10179
    Danusertib 827318-97-8 99.68%
    Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.
    Danusertib
  • HY-B0134A
    Bestatin hydrochloride 65391-42-6 99.94%
    Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.
    Bestatin hydrochloride
  • HY-N2334A
    Glycochenodeoxycholic acid sodium salt 16564-43-5 98.51%
    Glycochenodeoxycholic acid sodium salt (Sodium glycochenodeoxycholate) is a relatively toxic bile salt generated in the liver from chenodeoxycholic acid and glycine. Glycochenodeoxycholic acid sodium salt 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 sodium salt induces stemness and chemoresistance via activating STAT3 signaling pathway in hepatocellular carcinoma cells (HCC). Glycochenodeoxycholic acid sodium salt is promising for research in the field of cholestasis desease, hepatocellular carcinoma and primary sclerosing cholangitis (PSC).
    Glycochenodeoxycholic acid sodium salt
  • HY-139413
    β-D-Glucan 9041-22-9 99.00%
    β-D-glucan is a natural non-digestible polysaccharide and high biocompatibility that can be selectively recognized by recognition receptors such as Dectin-1 and Toll-like receptors as well as being easily internalized by murine or human macrophages, which is likely to attribute to a target delivery. β-d-glucan is an enteric delivery vehicle for probiotics.
    β-D-Glucan
  • HY-P9970A
    Infliximab (Anti-TNF-α) 99.00%
    Infliximab (Anti-TNF-α) (Avakine (Anti-TNF-α)) is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α. Infliximab (Anti-TNF-α) prevents the interaction of TNF-α with TNF-α receptor (TNFR1 and TNFR2). Infliximab (Anti-TNF-α) has the potential for autoimmune, chronic inflammatory diseases and diabetic neuropathy research.
    Infliximab (Anti-TNF-α)