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 (1377):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-32364
    3-arylisoquinolinamine derivative 1029008-71-6 99.10%
    3-arylisoquinolinamine derivative is a 3-arylisoquinolinamine derivative with antitumor activity.
    3-arylisoquinolinamine derivative
  • HY-124663
    CBK289001 1212663-24-5
    CBK289001 is a tartrate-resistant acid phosphatase (TRAP/ACP5) inhibitor. CBK289001 inhibits TRAP 5bMV, TRAP 5bOX and TRAP 5aOX with IC50s of 125 µM, 4.21 µM and 14.2 µM, respectively.
    CBK289001
  • HY-136476B
    Cu(II) protoporphyrin IX 14494-37-2
    Cu (II) Protoporphyrin IX is used as a negative control for Zn (II) Protoporphyrin (an inihibitor of heme oxygenase). Heme oxygenase has been implicated in tumor cell resistance to chemotherapy, reduction of free radical formation and inflammation, and associated with vascular repair.
    Cu(II) protoporphyrin IX
  • HY-13864
    PF-4989216 1276553-09-3 99.38%
    PF-4989216 is a potent and selective PI3Kα inhibitor with a Ki of 0.6 nM.
    PF-4989216
  • HY-156753
    NorA-IN-1 1389310-69-3
    NorA-IN-1 (Compound 16) is a NorA inhibitor. NorA-IN-1 inhibits NorA efflux pump in everted membrane vesicles. NorA-IN-1 can be used for research of multidrug resistance.
    NorA-IN-1
  • HY-161847
    HZ1 3030492-40-8 99.20%
    Anticancer agent 241 (HZ1) is an orally active first-in-class cyclin-dependent kinase like 3 (CDKL3)-specific inhibitor. Anticancer agent 241 shows a strong tumor-suppressing effect, and has the potential to overcome the resistance of CDK4/6 inhibitor.
    HZ1
  • HY-N3710
    Dehydrocrenatidine 65236-62-6 ≥98.0%
    Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain.
    Dehydrocrenatidine
  • HY-15889A
    AMG 925 (HCl) 1401034-19-2
    AMG 925 HCl is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
    AMG 925 (HCl)
  • HY-114982
    KEA1-97 2138882-71-8 98.05%
    KEA1-97 is a selective Thioredoxin-caspase 3 interaction disruptor (IC50=10 μM). KEA1-97 disrupts the interaction of thioredoxin with caspase 3, activates caspases, and induces apoptosis without affecting thioredoxin activity.
    KEA1-97
  • HY-158125
    PSMA binder-2 2149567-00-8
    PSMA binder-2 is a ligand for PSMA and can be used to synthesize Ac-PSMA-trillium. Ac-PSMA-trillium is a suitable PSMA-targeting compound with improved PSMA binding properties and pharmacokinetic properties. PSMA ligands have different biological applications after being modified 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).
    PSMA binder-2
  • HY-B1056
    Procodazole 23249-97-0 99.73%
    Procodazole is an orally active enhancer and a non-specific active immune protector against viral and bacterial infections. Procodazole also exhibits antiparasitic activity. In addition, Procodazole is a carbonic anhydrase inhibitor with antitumor activity.
    Procodazole
  • HY-125170
    Galiellalactone 133613-71-5
    Galiellalactone is a is a small non-toxic and non-mutagenic fungal metabolite, a selective inhibitor of STAT3 signaling, with an IC50 of 250-500 nM. Galiellalactone can be used to research castration-resistant prostate cancer.
    Galiellalactone
  • HY-161313
    DYB-03 2982792-85-6 99.49%
    DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 inhibits migration, invasion, and angiogenesis of lung cancer cells and HUVECs in vitro and in vivo. DYB-03 induces apoptosis in 2-ME2- and GSK126-resistant of A549 and H460 cells.
    DYB-03
  • HY-157169
    IBL-302 1414455-21-2 98.21%
    IBL-302 (AMU302) is an orally available dual-signaling inhibitor of PIM and PI3K/AKT/mTOR with activity against breast cancer and neuroblastoma. IBL-302 demonstrated in vivo efficacy in a nude mouse xenograft model, inhibiting trastuzumab (HY-P9907) resistance challenges. IBL-302 also enhances the effects of common cytotoxic chemotherapy drugs cisplatin (HY-17394), doxorubicin (HY-15142A), and etoposide (HY-13629).
    IBL-302
  • HY-104067
    Naphthol AS-MX phosphate 1596-56-1 99.50%
    Naphthol AS-MX phosphate (NASTRp) is a small molecule inhibitor of the CREB (cyclic adenosine phosphate reaction element binding protein)-CBP (CREB binding protein) transcription factor complex. Naphthol AS-MX phosphate shows antitumor activity against lung cancer cells, inhibiting tumor cell proliferation (IC50=3.701 μmol/L), colony formation, and anchored independent growth in soft AGAR. Naphthol AS-MX phosphate can be used in the study of KRAS mutated lung cancer, especially for KRAS mutated lung cancer with poor chemotherapy resistance and prognosis.
    Naphthol AS-MX phosphate
  • HY-U00244A
    Benzquinamide hydrochloride 113-69-9 99.14%
    Benzquinamide (P2647) is an antiemetic which can bind to the α2A, α2B, and α2C adrenergic receptors (α2-AR) with Ki values of 1,365, 691, and 545 nM, respectively. Benzquinamide also inhibits P-glycoprotein mediated drug efflux and potentiates anticancer agent cytotoxicity in multidrug resistant cells.
    Benzquinamide hydrochloride
  • HY-148574
    MCT1-IN-3 2878360-80-4 98.65%
    MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor with an IC50 value of 81.0 nM. MCT1-IN-3 has also significant inhibitivity against the multidrug transporter ABCB1. MCT1-IN-3 can be used for the research of cancer.
    MCT1-IN-3
  • HY-113973
    LPA2 antagonist 2 36840-10-5
    LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA3 (IC50 of 13.85 μM).
    LPA2 antagonist 2
  • HY-163940
    LX1 2647877-84-5 99.13%
    LX1 is an anti-prostate cancer compound that targets androgen receptor (AR), AR variants and steroidogenic enzyme AKR1C3. LX1 inhibits the enzymatic activity of AKR1C3, reduces the conversion of androstenedione to testosterone and reduces the expression of AR and AR-V7 and downregulates their target genes. LX1 overcomes the resistance of tumor cells to Enzalutamide (HY-70002), and the combination with Enzalutamide (HY-70002) further inhibits tumor growth.
    LX1
  • HY-111425
    SSE15206 1370046-40-4 99.88%
    SSE15206 is a microtubule polymerization inhibitor (GI50 = 197 nM in HCT116 cells) that overcomes multidrug resistance. Causes aberrant mitosis resulting in G2/M arrest due to incomplete spindle formation in cancer cells.
    SSE15206