D 927

Tocris Bioscience | Catalog # 8975

Molecular glue increasing the binding affinity of PI3Kα catalytic subunit p110α to canonical small guanosine triphosphatase RAS proteins
Tocris Bioscience
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Key Product Details

Description

Molecular glue increasing the binding affinity of PI3Kα catalytic subunit p110α to canonical small guanosine triphosphatase RAS proteins

Product Description

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. 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 insulin, 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.

Product Specifications for D 927

Molecular Weight

452.50

Formula

C23H21FN4O3S

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

3-Fluoro-4-[[7-[2-(2-methoxyethoxy)phenyl]thieno[2,3-d]pyridazin-4-yl]amino]benzeneacetamide

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.

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Solubility

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 452.50.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all 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 22.10 mL
5 mM 0.44 mL 2.21 mL 4.42 mL
10 mM 0.22 mL 1.10 mL 2.21 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Background References

References are publications that support the biological activity of the product.

Product Documents for D 927

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for D 927

For research use only

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