GNF-2

Name: GNF-2
Brand: MedChemExpress
SKU: HY-11007
Rating: 5.0 (2 reviews)

Cat. No.: HY-11007 Purity: 98.73%: FAQs
Data Sheet SDS COA Handling Instructions

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GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC₅₀ of 138 nM .

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

GNF-2 Chemical Structure

CAS No. : 778270-11-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 84	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 84	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 36	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 77	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 825	In-stock	Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE GNF-2

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Description

GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC₅₀ of 138 nM ^[1].

IC₅₀ & Target^[1]

Bcr-Abl

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	> 10 μM Compound: 2, GNF-2	Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing FIt3-ITD kinase assessed as proliferation after 48 hrs by MTT assay Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing FIt3-ITD kinase assessed as proliferation after 48 hrs by MTT assay	[PMID: 16415863]
BaF3	IC₅₀	> 10 μM Compound: 2, GNF-2	Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing Tel-PDGFRbeta kinase assessed as proliferation after 48 hrs by MTT assay Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing Tel-PDGFRbeta kinase assessed as proliferation after 48 hrs by MTT assay	[PMID: 16415863]
BaF3	IC₅₀	> 10 μM Compound: 2, GNF-2	Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing TPR-MET kinase assessed as proliferation after 48 hrs by MTT assay Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing TPR-MET kinase assessed as proliferation after 48 hrs by MTT assay	[PMID: 16415863]
BaF3	IC₅₀	> 10 μM Compound: 2, GNF-2	Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing Tel-JAK1 kinase assessed as proliferation after 48 hrs by MTT assay Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing Tel-JAK1 kinase assessed as proliferation after 48 hrs by MTT assay	[PMID: 16415863]
BaF3	IC₅₀	> 10000 nM Compound: 2, GNF-2	Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A337N mutant assessed as cell viability after 48 hrs by MTT assay Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A337N mutant assessed as cell viability after 48 hrs by MTT assay	[PMID: 16415863]
BaF3	IC₅₀	138 nM Compound: 2, GNF-2	Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl assessed as cell viability after 48 hrs by MTT assay Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl assessed as cell viability after 48 hrs by MTT assay	[PMID: 16415863]
BaF3	IC₅₀	2367 nM Compound: 2, GNF-2	Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A334l mutant assessed as cell viability after 48 hrs by MTT assay Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A334l mutant assessed as cell viability after 48 hrs by MTT assay	[PMID: 16415863]
HL-60	IC₅₀	> 10 μM Compound: 2, GNF-2	Antiproliferative activity against human HL60 Bcr-abl negative cells assessed as cell viability after 48 hrs by MTT assay Antiproliferative activity against human HL60 Bcr-abl negative cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 16415863]
Jurkat	IC₅₀	> 10 μM Compound: 2, GNF-2	Antiproliferative activity against human Jurkat Bcr-abl negative cells assessed as proliferation after 48 hrs by MTT assay Antiproliferative activity against human Jurkat Bcr-abl negative cells assessed as proliferation after 48 hrs by MTT assay	[PMID: 16415863]
K562	IC₅₀	0.273 μM Compound: 2, GNF-2	Antiproliferative activity against human K562 expressing Bcr-abl assessed as proliferation after 48 hrs by MTT assay Antiproliferative activity against human K562 expressing Bcr-abl assessed as proliferation after 48 hrs by MTT assay	[PMID: 16415863]
SUP-B15	IC₅₀	0.268 μM Compound: 2, GNF-2	Antiproliferative activity against human SUP-B15 expressing Bcr-abl assessed as proliferation after 48 hrs by MTT assay Antiproliferative activity against human SUP-B15 expressing Bcr-abl assessed as proliferation after 48 hrs by MTT assay	[PMID: 16415863]

In Vitro

GNF-2 selectively inhibits Bcr-abl-dependent cell proliferation. GNF-2 (0.005-10 μM; 48 hours) specifically inhibits the proliferation of the Bcr-abl-expressing cells with an IC₅₀ of 138 nM and not show any cytotoxic effects on the nontransformed cells at concentrations of up to 10 μM. GNF-2 (0.005-10 μM; 48 hours) causes a dose-dependent growth inhibition of the Bcr-abl-positive cell lines with IC₅₀ values of 273 nM (K562) and 268 nM (SUP-B15). GNF-2 (0.005-10 μM; 48 hours) inhibits E255V and Y253H mutant Bcr-abl cell growth (IC₅₀ values of 268 and 194 nM, respectively)^[1].
GNF-2 (1-10 μM; 48 hours) induces apoptosis of Bcr-abl-transformed cells^[1].
GNF-2 (0.1-10 μM; 90 minutes) inhibits the cellular tyrosine phosphorylation of Bcr-abl in a dose-dependent manner with an IC₅₀ of 267 nM^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	Ba/F3.p210, Ba/F3.p210^E255V and Ba/F3.p185^Y253H cells
Concentration:	0.005, 0.01, 0.1, 1, 10 μM
Incubation Time:	48 hours
Result:	Inhibited Bcr-abl-transformed cells proliferation.

Apoptosis Analysis^[1]

Cell Line:	Ba/F3.p210 and Ba/F3.p210^E255V cells
Concentration:	1, 10 μM
Incubation Time:	48 hours
Result:	Increased number of Ba/F3.p210 cells undergoing apoptosis at 1 μM for 48 h. Ba/F3.p210^E255V underwent apoptotic death after 48 h incubation in the presence of 1 μM or higher concentration.

Western Blot Analysis^[1]

Cell Line:	Ba/F3.p210 and Ba/F3.p210^E255V cells
Concentration:	0.1, 1, 10 μM
Incubation Time:	90 minutes
Result:	Decreased the autophosphorylation levels at a concentration of 1 μM and were barely detectable at 10 μM, whereas the level of total Bcr-abl remained unchanged. Induced a significant decrease in the levels of p-Stat5 (at Y694) at 1 μM in Ba/F3.p210 and Ba/F3.p210^E255V cells.

In Vivo

GNF-2 (10 mg/kg; i.p. for 8 days) protects LPS (5 mg/kg) induced bone erosion in mice. GNF-2 protects the LPS induced bone loss and abrogates the LPS-induced decreases of bone volume/tissue volume (BV/TV) of LPS-treated mice^[2].
GNF-2 prevents the LPS-induced increases of N.Oc/B.Pm, the percentage of Oc.S/BS, and the percentage of ES/BS^[2].

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

Animal Model:	Eight-week-old C57/BL6 mice were administered i.p. injections of LPS (5 mg/kg)^[2]
Dosage:	10 mg/kg
Administration:	I.p. injections for 8 days; 1 day before and every day after the LPS injection
Result:	Prevented inflammatory bone destruction in vivo.

Molecular Weight

374.32

Formula

C₁₈H₁₃F₃N₄O₂

CAS No.

778270-11-4

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=CC(C2=CC(NC3=CC=C(OC(F)(F)F)C=C3)=NC=N2)=C1)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (267.15 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6715 mL	13.3577 mL	26.7154 mL
5 mM	0.5343 mL	2.6715 mL	5.3431 mL
10 mM	0.2672 mL	1.3358 mL	2.6715 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.73%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (248 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

[1]. Adrián FJ, et al. Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol. 2006 Feb;2(2):95-102. [Content Brief]

[2]. Kim HJ, et al. The tyrosine kinase inhibitor GNF-2 suppresses osteoclast formation and activity. J Leukoc Biol. 2013 Oct 15. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6715 mL	13.3577 mL	26.7154 mL	66.7884 mL
	5 mM	0.5343 mL	2.6715 mL	5.3431 mL	13.3577 mL
	10 mM	0.2672 mL	1.3358 mL	2.6715 mL	6.6788 mL
	15 mM	0.1781 mL	0.8905 mL	1.7810 mL	4.4526 mL
	20 mM	0.1336 mL	0.6679 mL	1.3358 mL	3.3394 mL
	25 mM	0.1069 mL	0.5343 mL	1.0686 mL	2.6715 mL
	30 mM	0.0891 mL	0.4453 mL	0.8905 mL	2.2263 mL
	40 mM	0.0668 mL	0.3339 mL	0.6679 mL	1.6697 mL
	50 mM	0.0534 mL	0.2672 mL	0.5343 mL	1.3358 mL
	60 mM	0.0445 mL	0.2226 mL	0.4453 mL	1.1131 mL
	80 mM	0.0334 mL	0.1670 mL	0.3339 mL	0.8349 mL
	100 mM	0.0267 mL	0.1336 mL	0.2672 mL	0.6679 mL

GNF-2 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNF-2778270-11-4GNF2GNF 2Bcr-AblSARS-CoVSARS coronavirusallostericnon-ATP competitive inhibitorBa/F3.p210Ba/F3.p210^E255VBa/F3.p185^Y253Hbone erosionInhibitorinhibitorinhibit

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GNF-2

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GNF-2 Related Antibodies

2 Publications Citing Use of MCE GNF-2

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Complete Stock Solution Preparation Table

GNF-2 Related Classifications

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