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Gdc 0973

Manufactured by Selleck Chemicals
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GDC-0973 is a selective inhibitor of mitogen-activated protein kinase kinase (MEK). It functions by blocking the activation of the extracellular signal-regulated kinase (ERK) signaling pathway, which plays a crucial role in cell proliferation and survival.

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Lab products found in correlation

Plx4032, by Selleck Chemicals (4 mentions) Gsk2118436, by Selleck Chemicals (3 mentions) Gsk1120212, by Selleck Chemicals (3 mentions) Sorafenib, by Selleck Chemicals (2 mentions) Bez235, by Selleck Chemicals (2 mentions) Bkm120, by Selleck Chemicals (2 mentions) Cycloheximide (chx), by Merck Group (1 mentions) Doxycycline, by Merck Group (1 mentions) A 1155463, by Abbvie (1 mentions) Ci 1040, by Selleck Chemicals (1 mentions) S55746, by Selleck Chemicals (1 mentions) S63845, by Selleck Chemicals (1 mentions) Abt 737, by Selleck Chemicals (1 mentions) Venetoclax, by Abbvie (1 mentions) A 1210477, by Abbvie (1 mentions) Alectinib, by Selleck Chemicals (1 mentions) Celltiter glo luminescent cell viability assay, by Promega (1 mentions) Crizotinib, by Selleck Chemicals (1 mentions) Vemurafenib, by Selleck Chemicals (1 mentions) I bet151, by GlaxoSmithKline (1 mentions)

Spelling variants of this product

Cobimetinib (GDC-0973) (2 citations)

7 protocols using gdc 0973

1

Combinatorial Drug Screening Assay

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Venetoclax (VEN), A-1155463, and A-1210477 were provided by AbbVie. GDC-0973 (cobimetinib), CI1040, ABT-737, S63845, and S55746 were purchased from Selleckchem. Cycloheximide and doxycycline were purchased from Sigma-Aldrich.
Zhang Q., Riley-Gillis B., Han L., Jia Y., Lodi A., Zhang H., Ganesan S., Pan R., Konoplev S.N., Sweeney S.R., Ryan J.A., Jitkova Y., Dunner K J.r., Grosskurth S.E., Vijay P., Ghosh S., Lu C., Ma W., Kurtz S., Ruvolo V.R., Ma H., Weng C.C., Ramage C.L., Baran N., Shi C., Cai T., Davis R.E., Battula V.L., Mi Y., Wang J., DiNardo C.D., Andreeff M., Tyner J.W., Schimmer A., Letai A., Padua R.A., Bueso-Ramos C.E., Tiziani S., Leverson J., Popovic R, & Konopleva M. (2022). Activation of RAS/MAPK pathway confers MCL-1 mediated acquired resistance to BCL-2 inhibitor venetoclax in acute myeloid leukemia. Signal Transduction and Targeted Therapy, 7, 51.
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2

Generating Melanoma Resistance to BRAF Inhibitors

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To grow melanoma cells resistant to BRAFV600E inhibition, we exposed melanoma cells to 1 μM vemurafenib (PLX4032, Selleckchem S1267) for 2–3 weeks. For the BRAFV600E and MEK co-inhibition assays, we also used dabrafenib at 500 nM and 100 nM (GSK2118436, Selleckchem S2807), trametinib at 5 nM and 1 nM (GSK1120212, Selleckchem S2673), and cobimetinib at 10 nM and 1 nM (GDC-0973, Selleckchem S8041).
Torre E.A., Arai E., Bayatpour S., Jiang C.L., Beck L.E., Emert B.L., Shaffer S.M., Mellis I.A., Fane M.E., Alicea G.M., Budinich K.A., Weeraratna A.T., Shi J, & Raj A. (2021). Genetic screening for single-cell variability modulators driving therapy resistance. Nature genetics, 53(1), 76-85.
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3

Viability Assay of BRAF and ALK Mutants

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Vemurafenib, sorafenib, GDC-0973 (cobimetinib), crizotinib, and alectinib were purchased from Selleckchem (Houston, TX, USA). Drug studies were conducted in vitro using FACS-sorted, DAPI− eGFP+ Ba/F3 cells that stably expressed the MIGII-EV, MIGII-BRAF V600E, MIGII-RNF11-BRAF, and MIGII-KIF5B-ALK constructs using the CellTiter-Glo® Luminescent Cell Viability Assay from Promega Corporation (Madison, WI, USA), according to the manufacturer’s instructions. The MIGII-BRAF V600E, MIGII-RNF11-BRAF, and MIGII-KIF5B-ALK FACS-sorted Ba/F3 cells were maintained in RPMI + 10% Fetal Bovine Serum (FBS) + penicillin and streptomycin media without murine IL-3 while MIGII-EV was maintained in RPMI + 10% FBS + penicillin and streptomycin with recombinant murine IL-3 (1 ng/mL).
Diamond E.L., Durham B.H., Haroche J., Yao Z., Ma J., Parikh S.A., Wang Z., Choi J., Kim E., Cohen-Aubart F., Lee S.C., Gao Y., Micol J.B., Campbell P., Walsh M.P., Sylvester B., Dolgalev I., Aminova O., Heguy A., Zappile P., Nakitandwe J., Ganzel C., Dalton J.D., Ellison D.W., Estrada-Veras J., Lacouture M., Gahl W.A., Stephens P.J., Miller V.A., Ross J.S., Ali S.M., Briggs S.R., Fasan O., Block J., Héritier S., Donadieu J., Solit D.B., Hyman D.M., Baselga J., Janku F., Taylor B.S., Park C.Y., Amoura Z., Dogan A., Emile J.F., Rosen N., Gruber T.A, & Abdel-Wahab O. (2015). Diverse and Targetable Kinase Alterations Drive Histiocytic Neoplasms. Cancer discovery, 6(2), 154-165.
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4

Modulation of Cellular Signaling Cascades

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I-BET151 was supplied by GlaxoSmithKline (Brentford, UK). BMS-345541, BKM120, BEZ235, GSK1120212-(Trametinib), GDC0973-(Cobemitinib) UO126, PLX4032 (Vemurafenib), GSK2118436 (Dabrafenib), LY294002, were purchased from Selleck Chemicals (Houston, TX, USA). IFN-γ was from Shenandoah Biotechnologies (Warwick, PA, USA).
Gowrishankar K., Gunatilake D., Gallagher S.J., Tiffen J., Rizos H, & Hersey P. (2015). Inducible but Not Constitutive Expression of PD-L1 in Human Melanoma Cells Is Dependent on Activation of NF-κB. PLoS ONE, 10(4), e0123410.
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5

Generating Melanoma Resistance to BRAF Inhibitors

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To grow melanoma cells resistant to BRAFV600E inhibition, we exposed melanoma cells to 1 μM vemurafenib (PLX4032, Selleckchem S1267) for 2–3 weeks. For the BRAFV600E and MEK co-inhibition assays, we also used dabrafenib at 500 nM and 100 nM (GSK2118436, Selleckchem S2807), trametinib at 5 nM and 1 nM (GSK1120212, Selleckchem S2673), and cobimetinib at 10 nM and 1 nM (GDC-0973, Selleckchem S8041).
Torre E.A., Arai E., Bayatpour S., Jiang C.L., Beck L.E., Emert B.L., Shaffer S.M., Mellis I.A., Fane M.E., Alicea G.M., Budinich K.A., Weeraratna A.T., Shi J, & Raj A. (2021). Genetic screening for single-cell variability modulators driving therapy resistance. Nature genetics, 53(1), 76-85.
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6

Cell Proliferation Assay Using Chemical Compounds

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AZD6244, BKM120, BYL719, GDC0973, sorafenib, trametinib, BEZ235, Ku-0063794, RAD001, MK2206 and bosentan were obtained from Selleck Chemicals (Houston, TX). Carboplatin and 5-FU were obtained from Sigma. All stock solutions were prepared in DMSO (MP Biomedicals, Solon, OH) at a final concentration in culture media of 0.25% (v/v). Cells in 90 μl medium were seeded (3000 cells/well) onto 96-well microtitre plates (Nunc, Rochester, NY). After 24 hours, 10 μl of medium containing compounds in graded concentrations ranging from 0.1 μM to 1000 μM was added to the wells. Control wells contained 20 μl of relevant solvent to achieve a final concentration of 0.25% of each solvent. The effect on cell numbers was assessed using the CellTiter 96® AQueous Non-Radioactive Cell Proliferation Assay (Promega, Madison, WI) (MTS Assay) at 72 h post-treatment. The IC50 was calculated as the drug concentration that inhibited cell proliferation by 50% compared to vehicle controls as previously described [32 (link)].
Bhattacharya B., Low S.H., Chong M.L., Chia D., Koh K.X., Sapari N.S., Kaye S., Hung H., Benoukraf T, & Soong R. (2016). Acquired resistance to combination treatment through loss of synergy with MEK and PI3K inhibitors in colorectal cancer. Oncotarget, 7(20), 29187-29198.
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7

3D Co-culture Spheroid Assay for Drug Resistance

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To form a 3D co-culture cell spheroid, 5,000 RFP-tagged A375 or SK-MEL-24 cells were mixed with 5,000 GFP-tagged CAFs in one well of a U-bottomed 96-well plate (Thermo Fisher Scientific, Rochester, NY). Spheroid was formed by centrifuging the plate at 1,000 g for 10 minutes followed by incubation at 37°C in a humidified incubator with 5% CO 2 overnight. For drug resistance assay, spheroids were cultured using normal culture medium or medium (which was not certified by peer review) is the author/funder. All rights reserved. No reuse allowed without permission.
The copyright holder for this preprint this version posted February 18, 2021. ; https://doi.org/10.1101/2021.02.18.431841 doi: bioRxiv preprint containing 500 nM PLX4032 (Selleck Chemicals, Houston, TX) or 100 nM GDC0973 (Selleck Chemicals, Houston, TX) for 72 hours before they were collected for cell number counting. To count RFP+ melanoma cell number in the spheroids, 12 spheroids from each group were collected and digested using 2 mg/ml collagenase IV (Therma Fisher Scientific, MA) for one hour with stirring to generate a single cell suspension. A Countess II Automated Cell Counter (Thermo Fisher Scientific, Rochester, NY) was used to quantify melanoma cell number based on red fluorescence. Average melanoma cell number in each spheroid was calculated by dividing the total cell number by 12.
Liu T., Zhou L., Xiao Y., Andl T., & Zhang Y. (2021). BRAF inhibitors reprogram cancer-associated fibroblasts to drive matrix remodeling and therapeutic escape in melanoma.
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