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Results for "

castration-resistant

" in TargetMol Product Catalog
  • Inhibitors & Agonists
    43
    TargetMol | Inhibitors_Agonists
  • Inhibitory Antibodies
    4
    TargetMol | Inhibitory_Antibodies
  • Dye Reagents
    1
    TargetMol | Dye_Reagents
  • PROTAC Products
    7
    TargetMol | PROTAC
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    5
    TargetMol | Natural_Products
Y06137
T133632226534-49-0In house
Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.
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8-10 weeks
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MC-1-F2
T696592376894-10-7In house
MC-1-F2 is a direct FOXC2 inhibitor with anticancer activity, inhibits cancer stem cell (CSC) characteristics, and reduces the invasive ability of castration-resistant prostate cancer (CRPC) cell lines. MC-1-F2 can be used to study prostate cancer.
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4-6 weeks
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Bicalutamide
ICI-176334
T038090357-06-5
Bicalutamide (ICI-176334), a synthetic, nonsteroidal antiandrogen, competitively binds to cytosolic androgen receptors in target tissues, thereby inhibiting the receptor binding of androgens.
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Cabazitaxel
XRP6258, TXD 258, taxoid XRP6258, RPR-116258A
T2543183133-96-2
Cabazitaxel (taxoid XRP6258) is a taxane and antineoplastic agent which is currently used in the therapy of castration-resistant metastatic prostate cancer after failure of docetaxel.
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Abiraterone Acetate
Zytiga, CB7630
T6215154229-18-2
Abiraterone Acetate (CB7630) is an androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic castration-resistant PROSTATE CANCER.
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Bavdegalutamide
ARV-110
T222632222112-77-6
Bavdegalutamide (ARV-110) is an oral protein degrader that specifically binds to AR and mediates its degradation. Bavdegalutamide can degrade clinically relevant mutant AR proteins, maintain activity in a high androgen environment, and has an acceptable safety profile.
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Lupeol
Monogynol B, Farganasterol, Fagarasterol, Clerodol, (3β,13ξ)-Lup-20(29)-en-3-ol
T2895545-47-1
Lupeol (Monogynol B) is a novel androgen receptor inhibitor with anti-inflammatory and antioxidant activity.
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(S,R,S)-AHPC-Me hydrochloride
VHL ligand 2 hydrochloride, E3 ligase Ligand 1
T136711948273-03-7
(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is utilized in the synthesis of ARV-771, a potent BET protein degrader. It selectively degrades BET protein in castration-resistant cells with a DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, it serves as the VHL ligand from (S,R,S)-AHPC for recruiting von Hippel-Lindau (VHL) protein.
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TargetMol | Inhibitor Sale
(S,R,S)-AHPC-Me dihydrochloride
VHL ligand 2 dihydrochloride, E3 ligase Ligand 1 dihydrochloride, (S,R,S)-AHPC-Me dihydrochloride (1948273-02-6 free base)
T13671L
(S,R,S)-AHPC-Me dihydrochloride, also known as VHL ligand 2 dihydrochloride, is a chemical compound used in the synthesis of ARV-771. ARV-771 is a BET PROTAC degrader that relies on von Hippel-Landau (VHL) E3 ligase and exhibits potent degradation of BET proteins in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM. This compound acts as the VHL ligand, specifically the (S,R,S)-AHPC-based VHL ligand, facilitating the recruitment of von Hippel-Lindau (VHL) protein.
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EC1167
T179301610414-00-0
EC1169 is a targeted tubulysin conjugate that utilizes EC1167 as its linker. This compound shows promise in the treatment of recurrent metastatic, castration-resistant prostate cancer (MCRPC)[1].
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ZNU-IMB-Z15
T200015920915-26-0
Compound Z15 (ZNU-IMB-Z15) acts as an antagonist and degrader of the androgen receptor (AR). It inhibits the proliferation of castration-resistant prostate cancer (CRPC) cell lines that are AR-positive and induces apoptosis. Compound Z15 exhibits anticancer activity both in vivo and in vitro.
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4-6 weeks
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(+)-JJ-74-138
T2003192135545-34-3
(+)-JJ-74-138 is a novel non-competitive androgen receptor (AR) antagonist capable of inhibiting enzalutamide-resistant castration-resistant prostate cancer (CRPC).
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10-14 weeks
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XYD049
T2050223006788-11-7
XYD049 (compound 7d) is a CRBN-type molecular glue targeting GSPT1, with a DC50 of 19 nM, used for researching MYC-driven castration-resistant prostate cancer (CRPC). It effectively inhibits the growth of 22Rv1 cells (IC50 = 7 nM) and exhibits antitumor efficacy in vivo. XYD049 downregulates CRPC-associated oncogenes in 22Rv1 cells, including AR, AR-v7, PSA, and c-Myc. XYD049 comprises a molecular glue linker (black part) NH2-C5-NH-Boc, a CRBN-type E3 ligase ligand (blue part) Thalidomide 4-fluoride, and a target protein ligand (red part) GSPT1 ligand-1, with the E3 ligase ligand + linker forming the conjugate E3 Ligase Ligand-linker Conjugate 158.
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BKM1644
BKM 1644,BKM-1644
T268311070966-96-9
BKM1644 is an effective inhibition of the proliferation of metastatic, castration-resistant PCa (mCRPC) cells.
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IPI-9119
T368411346564-56-4
IPI-9119 is an orally active, selective, and irreversible FASN inhibitor (IC50 = 0.3 nM).
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Histone H3K27Me1 (23-34) (trifluoroacetate salt)
Histone H3K27Me1 (23-34) (trifluoroacetate salt)
T36980
Histone H3K27Me1 (23-34) is a peptide fragment of histone H3 that corresponds to amino acid residues 24-35 of the human histone H3.1 and H3.2 sequences. Monomethylation of histone H3 at lysine 27 is associated with actively transcribed genes and positively correlates with H3K36 trimethylation. Levels of H3K27Me1 are increased in tumor tissue isolated from patients with metastatic hormone-na ve and castration-resistant prostate cancer. Histone H3K27Me1 (23-34) has been used in epitope mapping of the lupus-derived monoclonal antibody BT164.
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Thailanstatin D
T390711609105-89-6
Thailanstatin D, an analogue of Thailanstatin A, inhibits AR-V7 gene splicing by disrupting the interaction between U2AF65 and SAP155, hindering their binding to the polypyrimidine tract situated between the branch point and the 3' splice site. This compound displays potent tumor inhibitory properties in human castration-resistant prostate cancer (CRPC) xenografts, resulting in cellular apoptosis.
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Orteronel
TAK-700, (S)-Orteronel
T6051566939-85-3
Orteronel ((S)-Orteronel)(TAK-700) was selected as a candidate for clinical evaluation. orteronel (TAK-700) is currently in phase III clinical trials for the treatment of castration-resistant prostate cancer.
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7-10 days
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HG122
T611091854976-77-4
HG122 is a chemical compound that effectively facilitates the degradation of androgen receptor (AR) via the proteasome pathway, leading to the inhibition of castration-resistant prostate cancer.
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6-8 weeks
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rucaparib hydrochloride
T61335773059-19-1
Rucaparib hydrochloride, also known as AG014699, is a powerful and orally active compound that inhibits PARP proteins including PARP-1, PARP-2, and PARP-3 with a Ki value of 1.4 nM for PARP1. Additionally, Rucaparib hydrochloride acts as a modest inhibitor of hexose-6-phosphate dehydrogenase (H6PD). This compound shows potential in research for castration-resistant prostate cancer (CRPC) [1] [2] [3] [4].
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1-2 weeks
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VPC-13789
T616532761146-51-2
VPC-13789 is a highly potent, selective, and orally bioavailable antiandrogen compound that shows promise for studying and developing therapeutics for castration-resistant prostate cancer (CRPC). In LNCaP cells, VPC-13789 effectively inhibits the transcriptional activity of the androgen receptor (AR) with an IC50 value of 0.19 μM [1].
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6-8 weeks
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rucaparib acetate
T61657773059-23-7
Rucaparib (AG014699) acetate is a highly effective oral inhibitor of PARP proteins, specifically targeting PARP-1, PARP-2, and PARP-3, with a Ki value of 1.4 nM for PARP1. Additionally, it exhibits inhibitory action on hexose-6-phosphate dehydrogenase (H6PD) to a moderate extent. Rucaparib acetate shows promise in the field of research for castration-resistant prostate cancer (CRPC). [1] [2] [3] [4]
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1-2 weeks
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MI-136
T68891628316-74-4
MI-136 inhibits expression of androgen receptor (AR) target genes that DHT induced.
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LLS30
T698742138367-58-3
LLS30 is an allosteric inhibitor of Galectin-1 (Gal-1). LLS30 decreases Gal-1 binding affinity to its binding partners, and potentially overcomes metastatic castration-resistant prostate cancer (mCRPC).
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6-8 weeks
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