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Apalutamide

Manufactured by Selleck Chemicals
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Apalutamide is a synthetic chemical compound used in laboratory research. It is a non-steroidal androgen receptor inhibitor. The core function of Apalutamide is to bind to and block the androgen receptor, which plays a role in the development and progression of certain types of cancer.

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Lab products found in correlation

Enzalutamide, by Selleck Chemicals (5 mentions) Darolutamide, by Selleck Chemicals (4 mentions) Karotinocyte sfm medium, by Thermo Fisher Scientific (2 mentions) Abiraterone acetate, by Selleck Chemicals (2 mentions) Dihydrotestosterone, by Merck Group (1 mentions) Dexamethasone (dex), by Selleck Chemicals (1 mentions) β estradiol, by Merck Group (1 mentions) Otx015, by Selleck Chemicals (1 mentions) Mifepristone, by Selleck Chemicals (1 mentions) R1881, by Merck Group (1 mentions) Lncap cells, by Merck Group (1 mentions) Dihydrotestosterone dht, by Merck Group (1 mentions) Charcoal stripped fbs, by Thermo Fisher Scientific (1 mentions) Hek293 cells, by Merck Group (1 mentions) 5α androstan 17β ol 3 one, by Merck Group (1 mentions) Rpmi 1640, by Thermo Fisher Scientific (1 mentions) Rapamycin, by Merck Group (1 mentions) Trametinib, by Selleck Chemicals (1 mentions) Mk2206, by MedChemExpress (1 mentions) Torin1, by Merck Group (1 mentions)

5 protocols using apalutamide

1

Prostate Cancer Compound Evaluation

Cited 2 times
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Apalutamide, darolutamide, dexamethasone, enzalutamide, mifepristone, OTX015, and JQ1 were purchased from Selleckchem. R1881, dihydrotestosterone (DHT), and beta-estradiol were purchased from Sigma-Aldrich. BET protein degrader ZBC260 and AR protein degrader ARD-61 were described previously (28 (link), 29 (link)).
Qiao Y., Wang X.M., Mannan R., Pitchiaya S., Zhang Y., Wotring J.W., Xiao L., Robinson D.R., Wu Y.M., Tien J.C., Cao X., Simko S.A., Apel I.J., Bawa P., Kregel S., Narayanan S.P., Raskind G., Ellison S.J., Parolia A., Zelenka-Wang S., McMurry L., Su F., Wang R., Cheng Y., Delekta A.D., Mei Z., Pretto C.D., Wang S., Mehra R., Sexton J.Z, & Chinnaiyan A.M. (2020). Targeting transcriptional regulation of SARS-CoV-2 entry factors ACE2 and TMPRSS2. Proceedings of the National Academy of Sciences of the United States of America, 118(1), e2021450118.
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2

Androgen receptor regulation via LSD1 inhibitors

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Cell lines were maintained in Dulbecco’s Modified Eagle’s Medium (HEK293 cells; Sigma) or Roswell Park Memorial Institute (RPMI) medium (LNCaP cells; Sigma) supplemented with 10% fetal bovine serum (FBS) with 4 mM (HEK293) or 2 mM (LNCaP) l-glutamine and 1 mM pyruvate. For experiments, LNCaP cells were incubated for 24 h and then media was changed to RPMI-1640 (phenol free; Life Technologies) supplemented, for the remainder of the experiment, with 10% charcoal stripped FBS (Life Technologies). Dihydrotestosterone (DHT) and 5α-Androstan-17β-ol-3-one were from Sigma-Aldrich; LSD1 inhibitors LSD1-C76 and HCI-2509 were from Xcess Biosciences; enzalutamide and apalutamide were from Selleckchem. Chemical inhibitors of LSD1 were synthesised, and a separate publication will describe full details of the preparation.
Regufe da Mota S., Bailey S., Strivens R.A., Hayden A.L., Douglas L.R., Duriez P.J., Borrello M.T., Benelkebir H., Ganesan A., Packham G, & Crabb S.J. (2018). LSD1 inhibition attenuates androgen receptor V7 splice variant activation in castration resistant prostate cancer models. Cancer Cell International, 18, 71.
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3

Comprehensive Compound Treatment Protocol

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CDK7 inhibitor-THZ1 (MedChemExpress, HY-80013A/CS-3168), R1881C-III (Sigma, R0908), Trametinib (Selleckchem, S2673), Enzalutamide (Selleckchem, S1250), Apalutamide (Selleckchem, S2840), Darolutamide (Selleckchem, S7559), MLN4924 (Sigma, 5.05477), Torin1 (Sigma, 475991), LY294002 (MedChemExpress, HY-10108), MK-2206 (MedChemExpress, HY-10358), MG132 (MedChemExpress, HY-13259), DT-061 (MedChemExpress, HY-112929), Cycloheximide (Sigma, 66-81-9) and Rapamycin (Sigma, 37094) were dissolved and aliquoted in DMSO (Sigma, D2650). EGF (Abcam, ab259398) was dissolved and aliquoted in water.
Rasool R.U., O’Connor C.M., Das C.K., Alhusayan M., Verma B.K., Islam S., Frohner I.E., Deng Q., Mitchell-Velasquez E., Sangodkar J., Ahmed A., Linauer S., Mudrak I., Rainey J., Zawacki K.P., Suhan T.K., Callahan C.G., Rebernick R., Natesan R., Siddiqui J., Sauter G., Thomas D., Wang S., Taylor D.J., Simon R., Cieslik M., Chinnaiyan A.M., Busino L., Ogris E., Narla G, & Asangani I.A. (2023). Loss of LCMT1 and biased protein phosphatase 2A heterotrimerization drive prostate cancer progression and therapy resistance. Nature Communications, 14, 5253.
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4

Characterization of Enzalutamide-Resistant Prostate Cell Lines

Cited 1 time
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C4–2B MDVR (C4–2B Enzalutamide resistant) and CWR22Rv1 cells were maintained in RPMI1640, whereas HEK293 and IMR90 fibroblast cells were cultured in DMEM supplemented with 10% fetal bovine serum (FBS), 100 units/ml penicillin, and 0.1 mg/ml streptomycin. RWPE-1 cells were grown in Karotinocyte SFM medium (Gibco). All cell line experiments were performed within six months of receipt from the ATCC or resuscitation after cryopreservation. C4–2B cells were kindly provided and authenticated by Dr. Leland Chung Lab at Cedars-Sinai Medical Center (Los Angeles, CA, USA). C4–2B MDVR cells were maintained in medium containing 20 μM Enzalutamide. Parental C4–2B cells were passaged alongside the resistant cells as an appropriate control [25 (link),26 ]. All cell lines were routinely tested as mycoplasma-free by PCR and authenticated using the short tandem repeat (STR) method. All cells were maintained at 37 °C in a humidified incubator with 5% carbon dioxide. Enzalutamide, apalutamide, darolutamide, and abiraterone acetate were purchased from Selleck Chemical. JG98 and JG231 were synthesized as described and their identities confirmed by 1H NMR and LC-MS/MS. Purity was > 95%, as determined by HPLC [27 (link)].
Xu P., Yang J.C., Ning S., Chen B., Nip C., Wei Q., Liu L., Johnson O.T., Gao A.C., Gestwicki J.E., Evans C.P, & Liu C. (2023). Allosteric inhibition of HSP70 in collaboration with STUB1 augments enzalutamide efficacy in antiandrogen resistant prostate tumor and patient-derived models. Pharmacological research, 189, 106692.
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5

Characterization of Enzalutamide-Resistant Prostate Cell Lines

Cited 1 time
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C4–2B MDVR (C4–2B Enzalutamide resistant) and CWR22Rv1 cells were maintained in RPMI1640, whereas HEK293 and IMR90 fibroblast cells were cultured in DMEM supplemented with 10% fetal bovine serum (FBS), 100 units/ml penicillin, and 0.1 mg/ml streptomycin. RWPE-1 cells were grown in Karotinocyte SFM medium (Gibco). All cell line experiments were performed within six months of receipt from the ATCC or resuscitation after cryopreservation. C4–2B cells were kindly provided and authenticated by Dr. Leland Chung Lab at Cedars-Sinai Medical Center (Los Angeles, CA, USA). C4–2B MDVR cells were maintained in medium containing 20 μM Enzalutamide. Parental C4–2B cells were passaged alongside the resistant cells as an appropriate control [25 (link),26 ]. All cell lines were routinely tested as mycoplasma-free by PCR and authenticated using the short tandem repeat (STR) method. All cells were maintained at 37 °C in a humidified incubator with 5% carbon dioxide. Enzalutamide, apalutamide, darolutamide, and abiraterone acetate were purchased from Selleck Chemical. JG98 and JG231 were synthesized as described and their identities confirmed by 1H NMR and LC-MS/MS. Purity was > 95%, as determined by HPLC [27 (link)].
Xu P., Yang J.C., Ning S., Chen B., Nip C., Wei Q., Liu L., Johnson O.T., Gao A.C., Gestwicki J.E., Evans C.P, & Liu C. (2023). Allosteric inhibition of HSP70 in collaboration with STUB1 augments enzalutamide efficacy in antiandrogen resistant prostate tumor and patient-derived models. Pharmacological research, 189, 106692.
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