[CAS NO. 1243245-18-2] GNF-6231

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PRODUCTS SPECIFICATIONS [1243245-18-2]

Catalog

HY-100408

Brand

MCE

CAS

1243245-18-2

DESCRIPTION [1243245-18-2]

Overview

MDL	MFCD30343851
Molecular Weight	448.49
Molecular Formula	C24H25FN6O2
SMILES	O=C(NC1=NC=C(N2CCN(C(C)=O)CC2)C=C1)CC3=CN=C(C4=CC(F)=NC=C4)C(C)=C3

For research use only. We do not sell to patients.

Summary

GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling. 1) GNF-6231 shows IC50s of greater than 10 μM on all CYP isoforms tested 2) GNF-6231 have favorable potency and a PK profile across preclinical species upon oral administration. 3) The reference for orally in MMTV-Wnt1 tumor bearing mice is dosed at 3 mg/kg. 4) GNF-6231 showed very robust dose-related antitumor efficacy.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 36 mg/mL ( 80.27 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2297 mL	11.1485 mL	22.2970 mL
5 mM	0.4459 mL	2.2297 mL	4.4594 mL
10 mM	0.2230 mL	1.1149 mL	2.2297 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 3 mg/mL (6.69 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 3 mg/mL (6.69 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 3 mg/mL (6.69 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Cheng D et al. Discovery of Pyridinyl Acetamide Derivatives as Potent, Selective, and Orally Bioavailable Porcupine Inhibitors. ACS Med Chem Lett. 2016 May 10;7(7):676-80.