GSK1059615
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MedKoo CAT#: 205739

CAS#: 958852-01-2

Description: GSK1059615 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor GSK1059615 inhibits PI3K in the PI3K/AKT kinase signaling pathway, which may trigger the translocation of cytosolic Bax to the mitochondrial outer membrane and an increase in mitochondrial membrane permeability, followed by apoptosis. Bax is a member of the proapoptotic Bcl-2 family of proteins. PIK3, an enzyme often overexpressed in cancer cells, plays a crucial role in tumor cell regulation and survival. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).


Chemical Structure

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GSK1059615
CAS# 958852-01-2

Theoretical Analysis

MedKoo Cat#: 205739
Name: GSK1059615
CAS#: 958852-01-2
Chemical Formula: C18H11N3O2S
Exact Mass: 333.06
Molecular Weight: 333.364
Elemental Analysis: C, 64.85; H, 3.33; N, 12.60; O, 9.60; S, 9.62

Price and Availability

Size Price Availability Quantity
10mg USD 150
25mg USD 250
50mg USD 450
100mg USD 650
200mg USD 950
500mg USD 1650
1g USD 2650
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Related CAS #: 958852-01-2   1356195-42-0 (sodium salt hydrate)  

Synonym: GSK1059615; GSK-1059615; GSK-1059615.

IUPAC/Chemical Name: (E)-4-((4-(pyridin-4-yl)quinolin-6-yl)methylene)thiazolidine-2,5-dione

InChi Key: SSROGLWTGKZPRA-MHWRWJLKSA-N

InChi Code: InChI=1S/C18H11N3O2S/c22-17-16(21-18(23)24-17)10-11-1-2-15-14(9-11)13(5-8-20-15)12-3-6-19-7-4-12/h1-10H,(H,21,23)/b16-10+

SMILES Code: O=C(N/C1=C/C2=CC=C3N=CC=C(C4=CC=NC=C4)C3=C2)SC1=O

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: >2 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:
Biological target: GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
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 333.36 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.

Recalculate based on batch purity %
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: 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 vivo 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.

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 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.