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 (1383):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-13701
    Nelarabine 121032-29-9 99.76%
    Nelarabine (506U78) is a nucleoside analogue and can be used for the research of T cell acute lymphoblastic leukemia (T-ALL).
    Nelarabine
  • HY-50671
    Zosuquidar trihydrochloride 167465-36-3 99.79%
    Zosuquidar (LY335979) trihydrochloride is a P-glycoprotein (P-gp) inhibitor (Ki=59 nM). Zosuquidar trihydrochloride shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research.
    Zosuquidar trihydrochloride
  • HY-19542
    C6 Ceramide 124753-97-5 99.82%
    C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects.
    C6 Ceramide
  • HY-B0719
    Ingenol Mebutate 75567-37-2 99.65%
    Ingenol Mebutate is an active ingredient in Euphorbia peplus, acts as a potent PKC modulator, with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity.
    Ingenol Mebutate
  • HY-12874
    CASIN 425399-05-9 99.89%
    CASIN is a selective GTPase Cdc42 inhibitor with an IC50 of 2 uM. CASIN can be used for the research of cancer.
    CASIN
  • HY-B0129
    Aztreonam 78110-38-0 99.64%
    Aztreonam (SQ-26,776) is a synthetic monocyclic beta-lactam antibiotic, which has a very high affinity for penicillin-binding protein 3 (PBP-3).
    Aztreonam
  • HY-10340
    Tirbanibulin 897016-82-9 99.45%
    Tirbanibulin (KX2-391) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
    Tirbanibulin
  • HY-77591
    Cysteamine hydrochloride 156-57-0 99.30%
    Cysteamine hydrochloride (2-Aminoethanethiol hydrochloride) is an orally active agent for the treatment of nephropathic cystinosis and an antioxidant.
    Cysteamine hydrochloride
  • HY-11079
    A-803467 944261-79-4 99.09%
    A-803467 is a potent and selective tetrodotoxin-resistant Nav1.8 sodium channel blocker (IC50=8 nM). A-803467 has shown significant anti-nociception in neuropathic and inflammatory pain models. A-803467 enhances the chemosensitivity of conventional anticancer agents through interaction with the ATP-binding cassette subfamily G member 2 (ABCG2) transporter.
    A-803467
  • HY-10484
    Pevonedistat hydrochloride 1160295-21-5 99.19%
    Pevonedistat (MLN4924) hydrochloride is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM. Pevonedistat hydrochloride induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat hydrochloride suppresses the growth of human tumour xenografts in mice.
    Pevonedistat hydrochloride
  • HY-101161
    SG3199 1595275-71-0 98.94%
    SG3199 is a cytotoxic DNA minor groove interstrand crosslinking pyrrolobenzodiazepine (PBD) dimer. SG3199 is the released warhead component of the ADC payload Tesirine (SG3249).
    SG3199
  • HY-147250
    Lirafugratinib 2549174-42-5 99.67%
    Lirafugratinib (RLY-4008) is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib covalently binds to Cys491. Lirafugratinib targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs.
    Lirafugratinib
  • HY-10426
    XCT790 725247-18-7 99.67%
    XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.
    XCT790
  • HY-108865
    Alteplase 105857-23-6
    Alteplase (Actilyse; Activase), a tissue plasminogen activator prepared by recombination, is a thrombolytic agent that play important roles in acute ischemic stroke, pulmonary embolism, acute myocardial infarction, and occluded catheters.
    The product size below only indicate the effective content of Alteplase. The ratio of Alteplase effective content : total content = 1:46-1:50. The actual ratio depends on the batch.)
    Alteplase
  • HY-104048
    QC6352 1851373-36-8 99.13%
    QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B).
    QC6352
  • HY-N0015
    Astragalin 480-10-4 99.94%
    Astragalin (Astragaline) a flavonoid with anti-inflammatory, antioxidant, anticancer, bacteriostatic activity. Astragalin inhibits cancer cells proliferation and migration, induces apoptosis. Astragalin is orally active and provides nerve and heart protection, and resistance against and osteoporosis.
    Astragalin
  • HY-108521
    HX531 188844-34-0 99.87%
    HX531 is an orally active RXR antagonist with an IC50 of 18 nM. HX531 upregulates the p53-p21Cip1 pathway. HX531 abrogates the anti-apoptotic effect of t-RA. HX531 exerts anti-obesity, anti-diabetic and anti-melanoma activities.
    HX531
  • HY-N0083
    Betulin 473-98-3 ≥98.0%
    Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line.
    Betulin
  • HY-B0965
    Thioridazine hydrochloride 130-61-0 99.96%
    Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
    Thioridazine hydrochloride
  • HY-15614
    SC144 895158-95-9 99.48%
    SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells.
    SC144