Loxo 101

Manufactured by Selleck Chemicals

Sourced in United States

LOXO-101 is a small molecule inhibitor. It functions by blocking the activity of specific enzymes.

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Lab products found in correlation

4 protocols using loxo 101

Colon Cancer Cell Line Apoptosis Assay

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Human colon cancer cell lines KM12SM, HT29, and HCT116 were obtained from the Korean Cell Line Bank (Seoul, Republic of Korea) and maintained in RPMI 1640 supplemented with 10% fetal bovine serum. The cells were cultured at 100% humidity and 5% CO₂ at 37 °C. The NTRK inhibitors LOXO-101, entrectinib, dovitinib, dovitinib lactate, dovitinib dilactic acid, regorafenib, and crizotinib were purchased from Selleck Chemicals (Houston, TX, USA). We used the annexin V-APC/propidium iodide (PI) apoptosis detection kit (Thermo Fisher Scientific, Rockford, IL, USA).

Sohn S.H., Sul H.J., Kim B., Kim B.J., Kim H.S, & Zang D.Y. (2021). TRK inhibitors block NFKB and induce NRF2 in TRK fusion-positive colon cancer. Journal of Cancer, 12(21), 6356-6362.

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GC Cell Line Maintenance and Compound Testing

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The human GC cell lines NCI-N87, SNU16, MKN7, MKN28, and AGS were obtained from the Korean Cell Line Bank (Seoul, Republic of Korea) and maintained in RPMI-1640 supplemented with 10% fetal bovine serum. The cells were cultured at 37 °C with 100% humidity and 5% CO₂. LOXO-101, entrectinib, dovitinib, dovitinib lactate, dovitinib dilactic acid, regorafenib, cabozantinib, and crizotinib were purchased from Selleck Chemicals (Houston, TX, USA).

Sohn S.H., Sul H.J., Kim B.J., Kim H.S, & Zang D.Y. (2021). Entrectinib Induces Apoptosis and Inhibits the Epithelial–Mesenchymal Transition in Gastric Cancer with NTRK Overexpression. International Journal of Molecular Sciences, 23(1), 395.

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Targeting YWHAE-NTRK3 Sarcoma with LOXO-101

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YWHAE-NTRK3-expressing murine sarcoma cells were treated with 50 nM of LOXO-101 (Selleck Chemicals, Houston, TX, USA) in vitro. Cells were seeded into 96-well plates at a concentration of 5 × 10³ cells per well and were treated with drugs for 72 h. XTT assays were then performed, and the half-maximal concentration (IC₅₀) was calculated. Fluorescence-activated cell sorting (FACS) analysis was performed for 24 h after treatment with drugs to detect Annexin-V- or EdU-positive fractions. For in vivo experiments, 1 × 10⁶ cells were transplanted subcutaneously into Balb/c nude mice, and the mice were treated with 100 mg/kg of LOXO-101 via oral administration daily, for seven days.

Teramura Y., Tanaka M., Yamazaki Y., Yamashita K., Takazawa Y., Ae K., Matsumoto S., Nakayama T., Kaneko T., Musha Y, & Nakamura T. (2020). Identification of Novel Fusion Genes in Bone and Soft Tissue Sarcoma and Their Implication in the Generation of a Mouse Model. Cancers, 12(9), 2345.

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Cell Culture and Compound Screening Protocol

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NCI-H2077, RT112, DMS114, NCI-H520 were cultured in RPMI media, supplemented with 10% FBS, and penicillin/streptomycin/L-glutamine (PSG). AN3 CA was cultured in Dulbecco’s Modified Eagle Medium (DMEM), supplemented with 10% FBS and PSG. All cell lines were cultured at 37 °C in a humidified chamber in the presence of 5% CO2. Cell lines were obtained from ATCC or Sigma-Aldrich, primarily in 2014 and 2016, and were not further authenticated. Cells were not passaged for more than 6 months and were routinely monitored in our laboratory for cellular morphology and microbial presence by microscopic observation. Cell lines used for ORF screen, gene expression and xenograft studies were tested and confirmed negative for Mycoplasma (MycoAlert PLUS, Lonza).
BGJ398(26 (link)), trametinib(27 (link)), LDC1267(28 (link)), LOXO-101 (ARRY-470)(29 (link)), imatinib(30 (link)), BKM120(31 (link)), AZD8931(32 (link)) and MGCD265 (glesatinib)(33 (link)) were purchased from Selleck. FIIN-3(34 (link)) and Torin2(35 (link)) were a generous gift from Dr. Nathanael Gray at Dana-Farber Cancer Institute (Boston, MA).

Bockorny B., Rusan M., Chen W., Liao R.G., Li Y., Piccioni F., Wang J., Tan L., Thorner A.R., Li T., Zhang Y., Miao C., Ovesen T., Shapiro G.I., Kwiatkowski D.J., Gray N.S., Meyerson M., Hammerman P.S, & Bass A.J. (2018). RAS-MAPK reactivation facilitates acquired resistance in FGFR1-amplified lung cancer and underlies a rationale for upfront FGFR-MEK blockade. Molecular cancer therapeutics, 17(7), 1526-1539.

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