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Taselisib

Manufactured by Genentech
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Taselisib is a lab equipment product manufactured by Genentech. It is a small molecule that functions as a kinase inhibitor, specifically targeting the phosphoinositide 3-kinase (PI3K) enzyme.

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Lab products found in correlation

Cyclin d1, by Cell Signaling Technology (1 mentions) C myc, by Cell Signaling Technology (1 mentions) Igf 1r, by Cell Signaling Technology (1 mentions) Phospho pras40thr246, by Cell Signaling Technology (1 mentions) Phospho erαser118, by Cell Signaling Technology (1 mentions) Phospho erαser167, by Cell Signaling Technology (1 mentions) Phospho p70s6k thr389, by Cell Signaling Technology (1 mentions) Cyclin e, by Cell Signaling Technology (1 mentions) Phospho mtor ser2448, by Cell Signaling Technology (1 mentions) Brca1, by Cell Signaling Technology (1 mentions) Cleaved parp, by Cell Signaling Technology (1 mentions) Phospho akt ser473, by Cell Signaling Technology (1 mentions) Phospho erk thr202 tyr204, by Cell Signaling Technology (1 mentions) Phospho s6 ser235 236, by Cell Signaling Technology (1 mentions) β actin antibody, by Merck Group (1 mentions) Gdc 0980, by Genentech (1 mentions) Venetoclax, by Abbvie (1 mentions) A 1210477, by Abbvie (1 mentions) Enzalutamide, by Astellas Pharma (1 mentions) Dimethyl sulfoxide (dmso), by Merck Group (1 mentions)

6 protocols using taselisib

1

Molecular Response to Taselisib and Letrozole

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Taselisib, also called GDC-0032, was generated at Genentech, Inc. (South San Francisco, CA). Letrozole was obtained from US Biological. Antibodies used include phospho-AKTSer473, AKT, phospho-PRAS40Thr246, phospho-S6Ser235/236, phospho-S6Ser240/242, S6, phospho-ERKThr202/Tyr204, ERK, phospho-ERαSer118, phospho-ERαSer167, cleaved PARP, p110α, phospho-p70S6KThr389, PR, cyclin E, phospho-mTORSer2448, IGF1R, BRCA1, c-Myc, CAV1, HER2 and cyclin D1 obtained from Cell Signaling (Danvers, MA). Antibodies for ERα and ERβ were obtained from Santa Cruz biotechnology (Santa Cruz, CA) and a βActin antibody was obtained from Sigma (St. Louis, MO).
Hoeflich K.P., Guan J., Edgar K.A., O'Brien C., Savage H., Wilson T.R., Neve R.M., Friedman L.S, & Wallin J.J. (2016). The PI3K inhibitor taselisib overcomes letrozole resistance in a breast cancer model expressing aromatase. Genes & Cancer, 7(3-4), 73-85.
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2

Single-Dose Taselisib Pharmacokinetics

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Taselisib (Genentech, Inc.) was taken on an empty stomach as a single
dose (powder-in-capsule formulation) at the same time of day +/- 2 hours
(33 (link)). The dose for each patient was
dependent on the dose level assignment.
Juric D., Krop I., Ramanathan R.K., Wilson T.R., Ware J.A., Sanabria Bohorquez S.M., Savage H.M., Sampath D., Salphati L., Lin R.S., Jin H., Parmar H., Hsu J.Y., Von Hoff D.D, & Baselga J. (2017). Phase I Dose Escalation Study of Taselisib (GDC-0032), an Oral PI3K Inhibitor, in Patients with Advanced Solid Tumors. Cancer discovery, 7(7), 704-715.
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3

Targeted Combination Therapy Evaluation

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Venetoclax and A-1210477 were provided by AbbVie (North Chicago, IL). GDC-0980, taselisib, and GDC-0491 were obtained from Genentech (South San Francisco CA).
Rahmani M., Nkwocha J., Hawkins E., Pei X., Parker R.E., Kmieciak M., Leverson J.D., Sampath D., Ferreira-Gonzalez A, & Grant S. (2018). Co-targeting BCL-2 and PI3K induces BAX-dependent mitochondrial apoptosis in AML cells. Cancer research, 78(11), 3075-3086.
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4

Taselisib and Enzalutamide for Prostate Cancer

Cited 1 time
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In the phase Ib, taselisib (supplied by Genentech, Inc.) was administered orally at a starting dose of 2 mg and escalated to 4 mg, 6 mg and 8 mg in a 3+3 trial design. This was in combination with 160 mg enzalutamide (supplied by Astellas Pharma, US) taken daily orally without interruption for a 28-day cycle. Patients were treated until disease progression or unacceptable toxicity. In phase II, patients received either 160 mg enzalutamide alone or 160 mg enzalutamide in combination with 4 mg taselisib orally, as prior phase I single agent testing of taselisib showed activity at 4 mg(21 (link)).
Lehmann B.D., Abramson V.G., Sanders M.E., Mayer E.L., Haddad T.C., Nanda R., Van Poznak C., Storniolo A.M., Nangia J., Gonzalez-Ericsson P.I., Sanchez V., Johnson K.N., Abramson R.G., Chen S.C., Shyr Y., Arteaga C.L., Wolff A.C, & Pietenpol J.A. (2019). TBCRC 032 IB/II Multicenter Study: Molecular insights to AR antagonist and PI3K inhibitor efficacy in patients with AR+ metastatic triple-negative breast cancer. Clinical cancer research : an official journal of the American Association for Cancer Research, 26(9), 2111-2123.
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5

Preparation of Taselisib Solution

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Taselisib was provided by Genentech Inc, South San Francisco, CA. In all experiments Taselisib was dissolved in dimethyl sulfoxide (Sigma-Aldrich, St. Louis, MO) as a 10 mM stock solution and diluted in culture medium immediately before use.
Lopez S., Schwab C.L., Cocco E., Bellone S., Bonazzoli E., English D.P., Schwartz P.E., Rutherford T., Angioli R, & Santin A.D. (2014). Taselisib, a selective inhibitor of PIK3CA, is highly effective on PIK3CA-mutated and HER2/neu amplified uterine serous carcinoma in vitro and in vivo. Gynecologic oncology, 135(2), 312-317.
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6

Cytotoxic Drug Preparation Protocol

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Paclitaxel was purchased from Selleck Chemicals (Selleckchem, Houston, TX, USA) and Chloroquine diphosphate salt from Sigma Aldrich. Taselisib (GDC0032) and ipatasertib (GDC-0068) were supplied by Genentech (Research proposal nr. OR-215703). They were dissolved in sterile dimethylsulfoxide (DMSO) and a 500 mM and 100 mM stock solutions, respectively, were prepared and stored in aliquots at −20 °C. Working concentrations were diluted in appropriate medium.
Cocco S., Leone A., Roca M.S., Lombardi R., Piezzo M., Caputo R., Ciardiello C., Costantini S., Bruzzese F., Sisalli M.J., Budillon A, & De Laurentiis M. (2022). Inhibition of autophagy by chloroquine prevents resistance to PI3K/AKT inhibitors and potentiates their antitumor effect in combination with paclitaxel in triple negative breast cancer models. Journal of Translational Medicine, 20, 290.
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