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 (1321):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-156628
    Opevesostat 2231294-96-3 99.79%
    Opevesostat (MK-5684; ODM-208) is an orally active and selective CYP11A1 inhibitor. Opevesostat has the potential for the research of metastatic castration-resistant prostate cancer (mCRPC).
    Opevesostat
  • HY-12744
    Genz-123346 free base 491833-30-8 99.80%
    Genz-123346 free base is an orally available inhibitor of glucosylceramide synthase. Genz-123346 blocks the conversion of ceramide to glucosylceramide (GL1) and inhibits GM1 with an IC50 of 14 nM.
    Genz-123346 free base
  • HY-121608
    Lumiflavin 1088-56-8 99.79%
    Lumiflavin (Lumiflavine), a riboflavine analog, causes significant inhibition of riboflavine uptake. Lumiflavin can effectively reduce the riboflavin enrichment in cancer stem-like cells (CSCs) and sensitize the effect of cisplatin Diamminedichloroplatinum (DDP) on CSCs. Lumiflavin is promising for research of ovarian cancer.
    Lumiflavin
  • HY-17010
    Retapamulin 224452-66-8 ≥98.0%
    Retapamulin (SB-275833) is a topical antibiotic that binds Staphylococcus aureus and E. coli ribosomes with a Kd of 3 nM. Retapamulin can be used in researches of atopic dermatitis and prostate cancer.
    Retapamulin
  • HY-100213
    EAI045 1942114-09-1 99.08%
    EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFRL858R, EGFRT790M and EGFRL858R/T790M at 10 μM ATP, respectively.
    EAI045
  • HY-19560
    SBI-0640756 1821280-29-8 99.75%
    SBI-0640756 (SBI-756) is an inhibitor of eIF4G1 and disrupts the eIF4F complex.
    SBI-0640756
  • HY-123611
    Supinoxin 888478-45-3 99.67%
    Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM.
    Supinoxin
  • HY-13068
    Golvatinib 928037-13-2 99.89%
    Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2/KDR/Flk-1 kinases with IC50s of 14 and 16 nM, respectively.
    Golvatinib
  • HY-136242
    UT-34 2168525-92-4 98.61%
    UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.
    UT-34
  • HY-N0240
    Herbacetin 527-95-7 99.70%
    Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects. Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis.
    Herbacetin
  • HY-150102
    EPI-7170 2139288-26-7 99.86%
    EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC).
    EPI-7170
  • HY-N2187
    Deoxyshikonin 43043-74-9 99.96%
    Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF. Deoxyshikonin inhibited colorectal cancer (CRC) through the PI3K/Akt/mTOR pathway. Deoxyshikonin has proangiogenesis effect and antitumor activity. Deoxyshikonin is an antibacterial agent against methicillin-resistant S. aureus (MRSA) and S. pneumonia (MIC=17 μg/mL).
    Deoxyshikonin
  • HY-B0140
    Aminophylline 317-34-0 99.90%
    Aminophylline is a competitive and non-selective phosphodiesterase (PDE) inhibitor. Aminophylline is a competitive adenosine receptor antagonist. Aminophylline has apulmonary vasodilator action as well as a bronchodilator action and has the potential for asthma research.
    Aminophylline
  • HY-70006
    Galeterone 851983-85-2 99.87%
    Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).
    Galeterone
  • HY-132166
    M4205 2590556-80-0 99.47%
    M4205 is a multi-target inhibitor for PDGFRB, PDGFRA, CSF1R, c-Kit, FLT3, and LCK, with an IC50s of 2.6, 50, 5.5, 44, 141 and 141 nM, respectively. M4205 exhibits antitumor efficacy in xenograft mouse models.
    M4205
  • HY-133017
    Amcenestrant 2114339-57-8 99.79%
    SAR439859 (compound 43d) is an orally active, non-steroidal, and selective estrogen receptor degrader (SERD). SAR439859 is an effective ER antagonist with ER degradation activity, an EC50 of 0.2 nM. SAR439859 can show potent anti-tumor effects and limited cross-resistance in ER+ breast cancer.
    Amcenestrant
  • HY-18299
    Purvalanol B 212844-54-7
    Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor CDK, with IC50s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity for CDK over a range of other protein kinases (IC50>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum.
    Purvalanol B
  • HY-148510
    HKB99 2414908-90-8
    HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1). HKB99 induces apoptosis. HKB99 inhibits the formation of invasive pseudopodia and inhibits migration. HKB99 increases the oxidative stress, activates JNK/c-Jun and suppresses AKT and ERK. HKB99 can be used for the research of non-small-cell lung cancer (NSCLC).
    HKB99
  • HY-B0362A
    Phentolamine mesylate 65-28-1 99.87%
    Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction.
    Phentolamine mesylate
  • HY-B1311
    Proadifen hydrochloride 62-68-0 99.98%
    Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases.
    Proadifen hydrochloride