GSK-1059615 sodium hydrate | CAS# 1356195-42-0 | PI3Kα inhibitor

MedKoo Cat#: 574713 | Name: GSK-1059615 sodium hydrate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

GSK1059615 is a potent, reversible, dual inhibitor of Class I PI3K isoforms (α, β, δ, and γ) and mTOR, with submicromolar IC₅₀ values: approximately 0.03 µM for PI3Kα, 0.06 µM for PI3Kβ, 0.19 µM for PI3Kγ, and 0.39 µM for PI3Kδ in biochemical assays. It also inhibits mTORC1 and mTORC2 activities, contributing to its broad anti-proliferative effects across a range of cancer cell lines. In cellular models, GSK1059615 reduces phosphorylation of downstream targets like Akt (Ser473 and Thr308), S6 ribosomal protein, and 4E-BP1, suppressing PI3K/Akt/mTOR signaling. It exhibits antiproliferative activity in vitro with GI₅₀ values in the low micromolar range in various human cancer cell lines, including breast, prostate, and colorectal cancers.

Chemical Structure

GSK-1059615 sodium hydrate

CAS#1356195-42-0 (sodium hydrate)

Theoretical Analysis

MedKoo Cat#: 574713

Name: GSK-1059615 sodium hydrate

CAS#: 1356195-42-0 (sodium hydrate)

Chemical Formula: C18H12N3NaO3S

Exact Mass: 0.0000

Molecular Weight: 373.36

Elemental Analysis: C, 57.91; H, 3.24; N, 11.25; Na, 6.16; O, 12.86; S, 8.59

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Related CAS #

958852-01-2 (free) 1356195-42-0 (sodium hydrate)

Synonym

GSK-1059615 sodium hydrate; GSK-1059615; GSK 1059615; GSK1059615;

IUPAC/Chemical Name

(5Z)-5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidinedione Sodium Salt Hydrate

InChi Key

KKSRFFGUIONCPS-FLPKAINGSA-M

InChi Code

InChI=1S/C18H11N3O2S.Na.H2O/c22-17-16(24-18(23)21-17)10-11-1-2-15-14(9-11)13(5-8-20-15)12-3-6-19-7-4-12;;/h1-10H,(H,21,22,23);;1H2/q;+1;/p-1/b16-10-;;

SMILES Code

O=C([N-]C/1=O)SC1=C/C2=CC=C3N=CC=C(C4=CC=NC=C4)C3=C2.[H]O[H].[Na+]

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

GSK-1059615 sodium salt hydrate is a potent inhibitor of PI 3-kinase α (PI3Kα).

In vitro activity:

In the primary OCC cells (all four lines, “OCC1-4”), treatment with GSK1059615 (3 μM, 24h) also inhibited cell proliferation, which was again indicated by BrdU ELISA OD reduction (Figure 2E). Collectively, these results imply that GSK1059615 inhibits human HNSCC cell proliferation. Reference: Oncotarget. 2017 Feb 7;8(31):50814-50823. https://pubmed.ncbi.nlm.nih.gov/28881606/

In vivo activity:

As demonstrated, i.p. daily administration of GSK1059615 at 30 mg/kg significantly inhibited SCC-9 tumor growth in the nude mice (Figure 6A). Estimated tumor growth, expressed as mm3 per day, was also dramatically inhibited with GSK1059615 administration (Figure 6B). The weight of GSK1059615-treated tumors was also dramatically lighter than those of vehicle control tumors (Figure 6C). Significantly, as shown in Figure 6A-6C, co-administration of cyclosporin A (5 mg/kg, i.v., daily), the cyclophilin-D inhibitor, largely attenuated GSK1059615-induced anti-SCC-9 tumor activity. Thus, mPTP and programmed necrosis pathway may also be required for GSK1059615-induced anti-tumor activity in vivo. Notably, cyclosporin A alone failed to inhibit SCC-9 tumor growth in the mice (Figure 6A-6C). Importantly, the mice body weight was not significantly different between the groups (Figure 6D), suggesting that these mice were well-tolerated to the tested regimens. Together, GSK1059615 inhibits SCC-9 tumor growth in nude mice, and its anti-tumor activity in vivo is compromised with co-administration of cyclosporin A. Reference: Oncotarget. 2017 Feb 7;8(31):50814-50823. https://pubmed.ncbi.nlm.nih.gov/28881606/

Preparing Stock Solutions

The following data is based on the product molecular weight 373.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Xie J, Li Q, Ding X, Gao Y. GSK1059615 kills head and neck squamous cell carcinoma cells possibly via activating mitochondrial programmed necrosis pathway. Oncotarget. 2017 Feb 7;8(31):50814-50823. doi: 10.18632/oncotarget.15135. PMID: 28881606; PMCID: PMC5584207.

In vitro protocol:

In vivo protocol:

1. Wei Q, Ramsey SA, Larson MK, et al. Elucidating the transcriptional program of feline injection-site sarcoma using a cross-species mRNA-sequencing approach. BMC Cancer. 2019;19(1):311. Published 2019 Apr 4. doi:10.1186/s12885-019-5501-z 2. Zellefrow CD, Sharlow ER, Epperly MW, et al. Identification of druggable targets for radiation mitigation using a small interfering RNA screening assay. Radiat Res. 2012;178(3):150-159. doi:10.1667/rr2810.1