| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C27H29FN8O3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GSK1838705A is a potent, reversible inhibitor of IGF-IR and the insulin receptor, with IC50 values of 2.0 nM and 1.6 nM, respectively, and it also inhibits ALK with an IC50 of 0.5 nM. It is supplied as a light yellow to yellow solid (C27H29FN8O3, MW 532.57) at 99.58% purity.
Physical & Chemical Properties
| CAS Number | 1116235-97-2 |
|---|---|
| Molecular Formula | C27H29FN8O3 |
| Molecular Weight | 532.57 g/mol |
| Purity | 99.58% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | FC1=C(C(NC)=O)C(NC2=C3C(NC=C3)=NC(NC4=CC5=C(CCN5C(CN(C)C)=O)C=C4OC)=N2)=CC=C1 |
| Signaling Pathway | Protein Tyrosine Kinase/RTK |
| Solubility | In Vitro: DMSO: ≥ 100 mg/mL (187.77 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 2.0 nM (IGF-IR), 1.6 nM (insulin receptor), 0.5 nM (ALK)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 100 mg/mL (187.77 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | 3 mg/mL (5.63 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 3 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (30.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Data provided by the manufacturer.
In Vitro
In cellular phosphorylation assays, GSK1838705A potently inhibits phosphorylation of IGF-IR and insulin receptor, with IC50s of 85 and 79 nM, respectively. The filter binding assay gives appKi values of 0.7 nM (IGF-IR) and 1.1 nM (insulin receptor). GSK1838705A inhibits proliferation across a panel of cell lines derived from solid and hematologic tumors. Its EC50s range from 20 nM to >8 μM; in most multiple myeloma and Ewing's sarcoma cell lines, they are <1 μM[1].
In Vivo
In animal xenograft models, GSK1838705A displays robust antitumor activity. Multiple myeloma, Ewing's sarcoma, and ALK-driven tumors (e.g., ALCL, NSCLC, and neuroblastoma) are the tumor types likely to respond to GSK1838705A. A single oral dose of GSK1838705A at 0.1 and 0.3 mg/kg gives 35% and 65% inhibition of IGF-IR phosphorylation, respectively, while doses ≥1 mg/kg completely inhibit ligand-induced IGF-IR phosphorylation[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Kinase Assay[1]
Use glutathione S-transferase–tagged proteins, expressed in baculovirus, that encode the intracellular domains of IGF-IR (amino acids 957–1367) and of IR (amino acids 979–1382) to determine IC50s by homogeneous time-resolved fluorescence assay. Determine appKi values by filter binding assay with activated IGF-IR and IR kinases. Carry out expanded kinase-selectivity profiling of GSK1838705A by screening the compound against the KinaseProfiler panel[1].
Cell Assay[1]
Seed cells in 96-well dishes, incubate overnight at 37°C, and treat with DMSO or GSK1838705A for 72 h. For NIH-3T3/LISN proliferation assays, seed cells on collagen-coated 96-well tissue culture plates and let them adhere for 24 h. Replace the medium with serum-free medium and treat the cells with GSK1838705A for 2 h. Add IGF-I (30 ng/mL) and incubate the cells for 72 h. Quantify cell proliferation with the CellTiter-Glo Luminescent Cell Viability Assay. Determine IC50s from cytotoxicity curves using a four-parameter curve fit software package[1].
Animal Administration[1]
Mice: Implant exponentially growing cells s.c. in the right flank of female nu/nu CD-1 or SCID mice, 8- to 12-wk-old. Dose the mice p.o. with the formulating vehicle or GSK1838705A. Weigh the mice and measure tumors with calipers twice weekly. Calculate tumor volumes[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Glucocorticoid receptor triggers a reversible drug-tolerant dormancy state with acquired therapeutic vulnerabilities in lung cancer. Nat Commun 2021 Jul 16;12(1):4360. PMID: 34272384
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. Sci Transl Med 2018 Jul 18;10(450):eaaq1093.
Aquaculture. 2025 Aug 15.
A Chemical Probe Strategy for Interrogating Inhibitor Selectivity Across the MEK Kinase Family. ACS Chem Biol 2017 May 19;12(5):1245-1256.
Urolithin C increases glucose-induced ERK activation which contributes to insulin secretion. Fundam Clin Pharmacol 2020 Oct;34(5):571-580.
T2DM inhibition of endothelial miR-342-3p facilitates angiogenic dysfunction via repression of FGF11 signaling. Biochem Biophys Res Commun 2018 Sep 3;503(1):71-78.
bioRxiv. 2023 May 14.
Patent. US20180263995A1.
