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.

Productos relacionados con Cancer Drug Resistance (1943):

Cat. No. Nombre del producto No. CAS Pureza Estructura química
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    RMS5 2497686-68-5
    RMS5, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS5 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS5 slightly diminishes the expression of the anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS5 has strong anticancer property.
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    Riviciclib 920113-02-6
    Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively. Riviciclib shows antitumor activity on cisplatin-resistant cells.
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    AZD4956 3045469-78-8
    AZD4956 is a potent and selective DNA polymerase theta (POLQ) inhibitor. AZD4956 exhibits an IC50 value of less than 3 μmol/L against POLQ and 3.4 μmol/L against MMEJ. AZD4956 suppresses the MMEJ pathway and enhances the activity of DNA-damaging agents in HRR-deficient cellular contexts. AZD4956 shows antitumor activity in BRCA1/2-mutated triple-negative breast cancer and prostate cancer models. AZD4956 can be used for the study of homologous recombination-deficient tumors.
    AZD4956
  • HY-13956B
    Pioglitazone potassium 1266523-09-4
    Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research.
    Pioglitazone potassium
  • HY-P10740
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    CBP-1018 is a PDC (peptide-drug conjugate) formed by conjugating Monomethyl auristatin E (HY-15162) to a dual-targeting ligand of FLOR1/PSMA (prostate-specific membrane antigen) via a linker (HY-78738). CBP-1018 binds to FLOR1 and prostate-specific membrane antigen (PSMA). CBP-1018 is applicable to the research of solid tumors and metastatic castration-resistant prostate cancer.
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  • HY-149918
    Antiproliferative agent-23 3049213-47-7
    Antiproliferative agent-23 is a microtubule-destabilizing agent (MDA) and efficiently disturbes the tubulin-microtubule system. Antiproliferative agent-23 induces apoptosis via a mitochondrion-dependent pathway by downregulating the Bcl-2 protein, upregulating Bax and Cyt c proteins, and activating the caspase cascade. Antiproliferative agent-23 initiates reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells (cisplatin resistant cancer cell line) via the PERK/ATF4/CHOP signaling pathway. Antiproliferative agent-23 has anti-tumor activity.
    Antiproliferative agent-23
  • HY-14661
    SB-743921 free base 618430-39-0
    SB-743921 free base is a potent selective inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM. SB-743921 free base can induce mitotic arrest, block cell cycle progression, induce apoptosis, and can be used in the research of myeloma, leukemia and other diseases.
    SB-743921 free base
  • HY-13646C
    Encequidar mesylate hydrochloride 2097125-58-9
    Encequidar (HM30181) mesylate hydrochloride is a potent and selective inhibitor of P-glycoprotein (MDR1). Encequidar mesylate hydrochloride improves anti-tumor efficacy of Paclitaxel (HY-B0015) in mouse tumor models.
    Encequidar mesylate hydrochloride
  • HY-108876
    Daunorubicin citrate 1884557-85-0
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    Daunorubicin citrate
  • HY-145584A
    Nesuparib hydrochloride 2055357-65-6
    Nesuparib (JPI-547) hydrochloride is the orally active inhibitor for PARP 1/2 and Tankyrase 1/2 that inhibits tankyrases 1, tankyrases 2, and PARP 1 with IC50s of 5, 1 and 2 nM, respectively. Nesuparib hydrochloride exhibits antitumor activity and can be used in research of advanced solid tumor.
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  • HY-183667
    JNJ-pan-AR 1332390-06-3
    JNJ-pan-AR is an orally active androgen receptor (AR) inhibitor with an IC50 of 19 nM and a Ki of 8.4 nM against human wild-type AR. JNJ-pan-AR abolishes androgen-induced KLK2 and KLK3 mRNA expression and reduces androgen-dependent colony formation in prostate cancer cells. JNJ-pan-AR blocks AR nuclear translocation, inhibits PSA protein expression, and represses the growth of AR-dependent tumor cells and ARF877L-driven tumor xenografts. JNJ-pan-AR blocks transactivation and signaling of wild-type AR and various mutant AR variants. JNJ-pan-AR is applicable for research on castration-resistant prostate cancer.
    JNJ-pan-AR
  • HY-12458
    Pyrindamycin A 118292-36-7
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    Pyrindamycin A
  • HY-B0532B
    Trifluoperazine dimaleate 605-75-4
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    Trifluoperazine dimaleate
  • HY-10617B
    Rucaparib hydrochloride 773059-19-1
    Rucaparib (AG014699) hydrochloride is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib hydrochloride is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib hydrochloride has the potential for castration-resistant prostate cancer (CRPC) research.
    Rucaparib hydrochloride
  • HY-135336AS1
    (S)-Verapamil-d6 (hydrochloride) 1329611-24-6
    (S)-Verapamil-d6 ((S)-(-)-Verapamil-d6) hydrochloride is the deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells.
    (S)-Verapamil-d<sub>6</sub> (hydrochloride)
  • HY-17367S3
    Atazanavir-d5 1132747-14-8
    Atazanavir-d5 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM.
    Atazanavir-d<sub>5</sub>
  • HY-17367S2
    Atazanavir-d9 1092540-51-6
    Atazanavir-d9 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM.
    Atazanavir-d<sub>9</sub>
  • HY-403733B
    (+)-JJ-450 1998094-24-8
    (+)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR) that inhibits AR nuclear localization and transcriptional activity in the absence of androgen. (+)-JJ-450 is less active than (-)-JJ-450 (HY-403733A) in inhibiting prostate-specific antigen (PSA) expression in LN95 cells, possibly because (+)-JJ-450 targets the ligand binding domain (LBD) of AR. (+)-JJ-450 inhibits the transcriptional activity of AR and its splice variants (e.g., ARv7) by promoting the degradation of unliganded AR in the nucleus and reducing the binding of AR to androgen response elements (AREs). (+)-JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to enzalutamide (MDV3100) (HY-70003).
    (+)-JJ-450
  • HY-173186
    TLK1-IN-1
    TLK1-IN-1 is a TLK1B inhibitor with a human IC50 of 7.2 μM. TLK1-IN-1 causes accumulation of DNA damage and induces apoptotic cell death in cancer cells. TLK1-IN-1 can be used for the research of metastatic castration-resistant prostate cancer.
    TLK1-IN-1
  • HY-151420
    Chitin synthase inhibitor 10 2725075-01-2
    Chitin synthase inhibitor 10 is a chitin synthase inhibitor. Chitin synthase inhibitor 10 shows excellent chitin synthase inhibitory activity with an IC50 value of 0.11 mM. Chitin synthase inhibitor 10 also is an antifungal agent and has significantly antifungal activity against drug-resistant fungal variants, such as C. albicans and C. neoformans. Chitin synthase inhibitor 10 can be used for the research of invasive fungal infections (IFIs).
    Chitin synthase inhibitor 10