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Submit ReviewD 927 New
Chemical Name: 3-Fluoro-4-[[7-[2-(2-methoxyethoxy)phenyl]thieno[2,3-d]pyridazin-4-yl]amino]benzeneacetamide
Purity: ≥98% (HPLC)
Biological Activity for D 927
D 927 is a molecular glue increasing the binding affinity of phosphoinositide 3-kinase α (PI3Kα) catalytic subunit p110α (Kd = 5.6 μM) to canonical small guanosine triphosphatase RAS proteins and to RRAS, RRAS2, and MRAS by three orders of magnitude.
D 927 binds to the RAS-binding domain of p110α, stabilizing the secondary structures of the PI3Kα in a RAS-binding conformation and forming direct interactions with RAS residues tyrosine-40 and arginine-41.
In vivo, D 927 mimicks the effects of insulin, rapidly lowering blood glucose concentrations, enhancing glucose metabolism in normal and Zucker fatty rats, and improving hyperglycemia in models of type 1 and type 2 diabetes, even in insulin-deficient diabetic animals. D 927 is orally bioavailable.
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Technical Data for D 927
| M. Wt | 452.5 |
| Formula | C23H21FN4O3S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2253733-37-6 |
| PubChem ID | 138454789 |
| InChI Key | GWLCNGUGZNFYHI-UHFFFAOYSA-N |
| Smiles | O=C(CC1=CC=C(C(F)=C1)NC2=C3C=CSC3=C(C4=CC=CC=C4OCCOC)N=N2)N |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for D 927
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 9.05 | 20 | |
| ethanol | 45.25 | 100 |
Preparing Stock Solutions for D 927
The following data is based on the product molecular weight 452.5. 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 | 2.21 mL | 11.05 mL | 22.1 mL |
| 5 mM | 0.44 mL | 2.21 mL | 4.42 mL |
| 10 mM | 0.22 mL | 1.1 mL | 2.21 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets for D 927
Certificate of Analysis is currently unavailable on-line.
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References for D 927
References are publications that support the biological activity of the product.
Terayama et al (2025) Molecular glues that facilitate RAS binding to PI3Ká promote glucose uptake without insulin. Science 389 402 PMID: 40705882
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Keywords: D 927, D 927 supplier, , Tocris Bioscience
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