PF-06928215

Alias: PF-06928215;PF 06928215;PF06928215
Cat No.:V4559 Purity: ≥98%
PF-06928215 (PF06928215) is a novel, potent,high affinity and selectivecGAS (cyclic GMP-AMP Synthase)inhibitor with the potential to be used for autoimmune diseases and inflammatory conditions.
PF-06928215 Chemical Structure CAS No.: 2378173-15-8
Product category: cGAS
This product is for research use only, not for human use. We do not sell to patients.
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25mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

PF-06928215 (PF06928215) is a novel, potent, high affinity and selective cGAS (cyclic GMP-AMP Synthase) inhibitor with the potential to be used for autoimmune diseases and inflammatory conditions. It inhibits cGAS with an IC50 of 4.9 μΜ. PF-06928215 is a high affinity (KD = 200 nM) active site-targeting, substrate-competitive cyclic GMP-AMP synthase (cGAS) inhibitor (IC50 = 4.9 μM; in the presence of 1 mM ATP, 0.3 mM GTP, 100 nM 45-bp interferon-stimulatory dsDNA (ISD)). PF-06928215 displays no inhibitory potency against dsDNA-induced IFN-β expression in cellular cGAS assays, most likely due to limited cell-permeability and/or high levels of cellular ATP and GTP in the reporter cells employed.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In the cellular cGAS experiment assessing dsDNA-induced IFN-β production, PF-06928215 did not exhibit any action [1].
References
[1]. Hall J, et al. Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay. PLoS One. 2017 Sep 21;12(9):e0184843.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H20N4O4
Molecular Weight
380.3972
CAS #
2378173-15-8
SMILES
O([H])C([C@]1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[C@]1([H])N([H])C(C1=C([H])N([H])N2C(C([H])=C(C3C([H])=C([H])C([H])=C([H])C=3[H])N=C21)=O)=O)=O
Synonyms
PF-06928215;PF 06928215;PF06928215
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~33.33 mg/mL (~87.62 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6288 mL 13.1441 mL 26.2881 mL
5 mM 0.5258 mL 2.6288 mL 5.2576 mL
10 mM 0.2629 mL 1.3144 mL 2.6288 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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