[CAS NO. 778277-15-9] GNF-5

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PRODUCTS SPECIFICATIONS [778277-15-9]

Catalog

HY-15738

Brand

MCE

CAS

778277-15-9

DESCRIPTION [778277-15-9]

Overview

MDL	MFCD16877246
Molecular Weight	418.37
Molecular Formula	C20H17F3N4O3
SMILES	FC(F)(F)OC(C=C1)=CC=C1NC2=NC=NC(C3=CC=CC(C(NCCO)=O)=C3)=C2

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

3 Publications Citing Use of MCE

Summary

GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC ₅₀ value of 0.22 µM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer ^[1] ^[2] .

IC50 & Target

IC50: 0.22 µM (Abl) ^[1]

In Vitro

GNF-5 has inhibition of wild-type Abl with an IC ₅₀ value of 0.22 µM but no inhibition for myristate site mutant E505K (IC ₅₀ ＞10 µM) ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay ^[1]

Cell Line:	wild type and mutant Bcr-Abl expressing Ba/F3 cells
Concentration:	0.2, 0.8 and 1.6 μM
Incubation Time:	48 h
Result:	Inhibited wild-type Abl in a non-ATP competitive fashion.

In Vivo

GNF-5 (5 mg/kg iv. or 20 mg/kg oral) has suitable pharmacokinetic parameters ^[1] .
GNF-5 (oral, 50 or 100 mg/kg, twice daily, for 7 days) shows efficacious in vivo but can observe relapses ^[1] .
GNF-5 (75 mg/kg, b.i.d) inhibits T315I Bcr-Abl combination with nilotinib in vivo ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male Balb/c mice ^[1]

Dosage:

5 mg/kg, 20 mg/kg

Administration:

5 mg/kg intravenously or 20 mg/kg orally

Result:

AUC_inf (min*ug/mL)	292.37
AUC_inf (hrs*nM	11647
C _max (nM)	4386.08
T _max (hrs)	0.50
Clast (nM)	636.16
T _1/2 (hrs)	2.30
V _ss (L/kg)	9.18
F (%)	44.82

Animal Model:	p210 xenograft model ^[1]
Dosage:	50 or 100 mg/kg
Administration:	oral, twice daily, for 7 days
Result:	Could normalize blood counts and spleen size.

Animal Model:	Bone marrow transduction/transplantation model ^[1]
Dosage:	75 mg/kg
Administration:	twice daily
Result:	Showed no significant response (alone). Showed no toxicity and had a strong and sustained inhibition of Bcr-Abl-mediated signaling combination with nilotinib.

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 : ≥ 49 mg/mL ( 117.12 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3902 mL	11.9511 mL	23.9023 mL
5 mM	0.4780 mL	2.3902 mL	4.7805 mL
10 mM	0.2390 mL	1.1951 mL	2.3902 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: ≥ 2.5 mg/mL (5.98 mM); Clear solution
2.

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

Solubility: ≥ 2.5 mg/mL (5.98 mM); Clear solution
3.

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

Solubility: ≥ 2.5 mg/mL (5.98 mM); Clear solution

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