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Samotolisib

Catalog No. T6883 CAS 1386874-06-1

Synonyms: GTPL8918, LY3023414

Samotolisib (LY3023414) is an oral ATP competitive inhibitor of the class I PI3K isoforms, DNA-PK, and mTOR. Samotolisib (LY3023414) has been used in trials studying the treatment of Neoplasm, Solid Tumor, COLON CANCER, BREAST CANCER, and Advanced Cancer, among others.

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Samotolisib, CAS 1386874-06-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 44.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 117.00
25 mg	In stock	$ 258.00
50 mg	In stock	$ 450.00
100 mg	In stock	$ 663.00
1 mL * 10 mM (in DMSO)	In stock	$ 78.00

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Purity: 99.71%

Purity: 99.61%

Purity: 99.06%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Samotolisib (LY3023414) is an oral ATP competitive inhibitor of the class I PI3K isoforms, DNA-PK, and mTOR. Samotolisib (LY3023414) has been used in trials studying the treatment of Neoplasm, Solid Tumor, COLON CANCER, BREAST CANCER, and Advanced Cancer, among others.
Targets&IC50	mTOR:165 nM, PI3Kγ:23.8 nM, PI3Kα:6.07 nM, DNA-PK:4.24 nM, PI3Kβ:77.6 nM, PI3Kδ:38 nM
In vitro	LY3023414 shows high solubility across a wide pH range. In vitro, inhibition of PI3K/AKT/mTOR signaling by LY3023414 causes G1 cell-cycle arrest and resulted in broad antiproliferative activity in cancer cell panel screens. In cell-based assays, LY3023414 inhibition of PI3K and mTOR is assessed in the PTEN-deficient U87 MG glioblastoma cell line. LY3023414 inhibits the phosphorylation of AKT at position T308 downstream of PI3K at an IC50 of 106 nM. Similarly, LY3023414 inhibits phosphorylation of AKT at position S473 (IC50 = 94.2 nM) by mTORC2 as well as phosphorylation of mTORC1 kinase targets p70S6K (position T389; IC50 =10.6 nM) and 4E-BP1 (positions T37/46; IC50 = 187 nM). The downstream phosphorylation of S6RP at positions pS240/244 (IC50 = 19.1 nM) by p70S6K was inhibited as well, indicating target inhibition along the entire PI3K/AKT/mTOR pathway by LY3023414[1].
In vivo	In vivo, LY3023414 demonstrates high bioavailability and dose-dependent dephosphorylation of PI3K/AKT/mTOR pathway downstream substrates such as AKT, S6K, S6RP, and 4E-BP1 for 4 to 6 hours, reflecting the drug's half-life of 2 hours. Intermittent target inhibition is sufficient for its antitumor activity. LY3023414 shows time- and dose-dependent target inhibition in vivo. It is currently being evaluated in phase 1 and 2 trials for the treatment of human malignancies[1].
Kinase Assay	Western blot analysis: The phosphorylation status of c-Met and VEGFR-2 is detected by Western blot analysis. For c-Met, MKN45 cells are incubated with a serial dilution of E7050 in complete medium at 37 °C for 2 h. For VEGFR-2, HUVEC are starved with human endothelial serum free medium containing 0.5% FBS for 24 h. Subsequently HUVEC are incubated with a serial dilution of E7050 for 1 h and then incubated with 20 ng/mL of human VEGF for 5 min. Cells are lysed by lysis buffer (50 mM HEPES [pH 7.4], 150 mM NaCl, 10% glycerol, 1% Triton X-100, 1.5 mM MgCl2, 1 mM EDTA [pH 8.0], 100 mM NaF, 1 mM phenylmethylsulfonyl fluoride 1 mM sodium orthovanadate, 10 μg/mL aprotinin, 50 μg/mL leupeptin, and 1 μg/mL pepstatin A). The resected tumor samples are homogenized with lysis buffer containing 25 mM β-glycerophosphate and 0.5% (v/v) phosphatase inhibitor cocktail 2 at 4 °C. Cellular debris is removed by centrifugation at 17 860 g for 20 min at 4 °C. Aliquots of the supernatants containing 5-20 μg of protein are subjected to SDS-PAGE under reducing conditions. The proteins are then transferred onto PVDF membranes, blocked with TBS containing 0.05% Tween-20 and either 5% skim milk or 5% BSA. The membranes are probed with the following antibodies: anti-c-Met polyclonal antibody (C-28) and anti-VEGFR-2 polyclonal antibody (C-20); mouse anti-phosphotyrosine clone 4 g10; and anti-VEGFR-2 polyclonal antibody, anti-phospho-VEGFR-2 (Tyr996) polyclonal antibody, and anti-phospho-c-Met (Tyr1234/1235) polyclonal antibody. Detection is performed using a Super Signal enhanced chemiluminescence kit. Immunoreactive bands are visualized by chemiluminescence with an Image Master-VDS-CL detection system. The intensity of each band is measured by using an image analyzer.

Synonyms	GTPL8918, LY3023414
Molecular Weight	406.48
Formula	C23H26N4O3
CAS No.	1386874-06-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 57 mg/mL (140.2 mM)

DMSO: 44 mg/mL (108.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Smith MC, et al. Mol Cancer Ther. 2016, [Epub ahead of print]

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Kinase Inhibitor Library Glycolysis Compound Library Anti-Aging Compound Library Angiogenesis related Compound Library Pediatric Drug Library

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Related compounds with same targets

IC 86621 SF2523 Wortmannin KU-0060648 Pictilisib dimethanesulfonate PIK-90 DMNB Compound 401

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Keywords

Samotolisib 1386874-06-1 Autophagy DNA Damage/DNA Repair PI3K/Akt/mTOR signaling DNA-PK mTOR PI3K Inhibitor GTPL8918 Phosphoinositide 3-kinase LY3023414 DNA-dependent protein kinase inhibit LY-3023414 GTPL-8918 GTPL 8918 LY 3023414 Mammalian target of Rapamycin inhibitor

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