GNF-7

Name: GNF-7
Brand: MedChemExpress
SKU: HY-10943
Rating: 5.0 (2 reviews)

Cat. No.: HY-10943 Purity: 99.70%: FAQs
Data Sheet SDS COA Handling Instructions

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GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC₅₀s of 133 nM and 61 nM for Bcr-Abl^WT and Bcr-Abl^T315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC₅₀s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies.

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

GNF-7 Chemical Structure

CAS No. : 839706-07-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 130	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 130	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 108	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 360	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 560	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 895	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE GNF-7

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Biological Activity
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References
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Description

IC₅₀ & Target

IC50: 133 nM (Bcr-Abl^WT)^[1], 61 nM (Bcr-Abl^T315I)^[1], 25 nM (ACK1)^[3], 8 nM (GCK)^[3]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	0.005 μM Compound: 27; GNF-7	Inhibition of Tel-ABL (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of Tel-ABL (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.014 μM Compound: 27; GNF-7	Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.12 μM Compound: 6; GNF-7	Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo or CCK-8 assay Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 28140585]
BaF3	GI₅₀	0.12 μM Compound: 27; GNF-7	Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	1.033 μM Compound: GNF-7	Growth inhibition of parental mouse BA/F3 cells after 72 hrs by celltiter-glo assay Growth inhibition of parental mouse BA/F3 cells after 72 hrs by celltiter-glo assay	[PMID: 30153003]
BaF3	IC₅₀	3.15 nM Compound: 4, GNF-7	Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	6.18 nM Compound: 4, GNF-7	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
HT-29	EC₅₀	100 nM Compound: GNF-7; 9	Anti-necroptic activity in TSZ induced necroptosis in human HT-29 cells pretreated with compound followed by TSZ stimulation for 8 hrs by celltiter-glo luminescent cell viability assay Anti-necroptic activity in TSZ induced necroptosis in human HT-29 cells pretreated with compound followed by TSZ stimulation for 8 hrs by celltiter-glo luminescent cell viability assay	[PMID: 36346971]
K562	GI₅₀	0.009 μM Compound: 27; GNF-7	Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
K562	IC₅₀	0.44 nM Compound: 4, GNF-7	Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay	[PMID: 23088644]
K562	IC₅₀	2.6 nM Compound: 4, GNF-7	Antiproliferative activity against imatinib-resistant human K562 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay Antiproliferative activity against imatinib-resistant human K562 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
KU812 cell line	IC₅₀	0.08 nM Compound: 4, GNF-7	Antiproliferative activity against human KU812 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay Antiproliferative activity against human KU812 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay	[PMID: 23088644]
OCI-AML-3	GI₅₀	0.219 μM Compound: GNF-7	Growth inhibition of human OCI-AML3 cells harboring NRAS-Q61L mutant after 72 hrs by celltiter-glo assay Growth inhibition of human OCI-AML3 cells harboring NRAS-Q61L mutant after 72 hrs by celltiter-glo assay	[PMID: 30153003]
U-937	GI₅₀	4.377 μM Compound: GNF-7	Growth inhibition of parental human U937 cells after 72 hrs by celltiter-glo assay Growth inhibition of parental human U937 cells after 72 hrs by celltiter-glo assay	[PMID: 30153003]

In Vitro

GNF-7 potently inhibits wild-type Bcr-Abl (IC₅₀<5 nM) and Bcr-Abl mutants such as T315I (IC₅₀=11 nM), G250E (IC₅₀<5 nM), E255V (IC₅₀=10 nM), F317L (IC₅₀<5 nM) and M351T (IC₅₀<5 nM) in cellular assays^[2].
GNF-7 (1 μM; 2 hours) suppresses AKT/mTOR signaling and GCK downstream^[3].
GNF-7 (1 μM; 24 hours) induces of apoptosis and cell cycle arrest in NRAS mutant cell lines^[3].

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

Western Blot Analysis^[3]

Cell Line:	Ba/F3-NRAS-G12D cells, OCI-AML3 cells
Concentration:	1 μM
Incubation Time:	2 hours
Result:	Caused a decreased level of phosphorylation of p70S6K1, AKT (S473), JNK, and p38.

Apoptosis Analysis^[3]

Cell Line:	OCI-AML3 cells
Concentration:	1 μM
Incubation Time:	24 hours
Result:	Increased the levels of both cleaved PARP and cleaved caspase 3 and diminished bcl-2 and MCL1.

Cell Cycle Analysis^[3]

Cell Line:	OCI-AML3 cells
Concentration:	1 μM
Incubation Time:	24 hours
Result:	Induced of G0-G1 arrest.

In Vivo

GNF-7 (10-20 mg/kg; o.p.; daily; for 7 days) displays significant in vivo efficacy against T315I Bcr-Abl in the bioluminescent xenograft mouse model^[2].
GNF-7 exhibits moderate oral bioavailability (mice 36%) and C_max (mice 3616 nM) following oral administration (mice 20 mg/kg)^[2].
GNF-7 exhibits terminal elimination half-lives (mice 3.8 h) due to high plasma clearance (8.6 mL/min/kg) following intravenous injection (mice 5 mg/kg)^[2].

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

Animal Model:	6-8 weeks old SCID beige female mice, with Ba/F3-T315I-Bcr-Abl cells xenograft^[2]
Dosage:	10 mg/kg, 20 mg/kg
Administration:	Oral administration, daily, for 7 days
Result:	Effectively inhibited tumor growth of T315I-Bcr-Abl-Ba/F3 cells in mice at low doses (10 mg/kg).

Animal Model:	5-6 weeks old male Balb/c mice (20-25 g)^[2]
Dosage:	5 mg/kg for i.v.; 20 mg/kg for i.g. (Pharmacokinetic Analysis)
Administration:	Intravenous injection and oral gavage
Result:	Oral bioavailability (36%), C_max (3616 nM), T_1/2 (3.2 h).

Molecular Weight

547.53

Formula

C₂₈H₂₄F₃N₇O₂

CAS No.

839706-07-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(C)C(N2CC3=CN=C(NC4=CC=C(C)N=C4)N=C3N(C)C2=O)=C1)C5=CC=CC(C(F)(F)F)=C5

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 : 20 mg/mL (36.53 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8264 mL	9.1319 mL	18.2638 mL
5 mM	0.3653 mL	1.8264 mL	3.6528 mL
10 mM	0.1826 mL	0.9132 mL	1.8264 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.

Molarity Calculator
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 mg/mL (3.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (3.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (3.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2 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 (20.0 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: 99.70%

Select Batch:

Data Sheet (277 KB) SDS (479 KB)

COA (245 KB) HNMR (274 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Lu X, et al. Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3458-63. [Content Brief]

[2]. Choi HG, et al. A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl. J Med Chem. 2010 Aug 12;53(15):5439-48. [Content Brief]

[3]. Cho, H., et al. First SAR study for overriding NRAS mutant driven acute myeloid leukemia. Journal of Medicinal Chemistry. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8264 mL	9.1319 mL	18.2638 mL	45.6596 mL
	5 mM	0.3653 mL	1.8264 mL	3.6528 mL	9.1319 mL
	10 mM	0.1826 mL	0.9132 mL	1.8264 mL	4.5660 mL
	15 mM	0.1218 mL	0.6088 mL	1.2176 mL	3.0440 mL
	20 mM	0.0913 mL	0.4566 mL	0.9132 mL	2.2830 mL
	25 mM	0.0731 mL	0.3653 mL	0.7306 mL	1.8264 mL
	30 mM	0.0609 mL	0.3044 mL	0.6088 mL	1.5220 mL

GNF-7 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-7839706-07-9GNF7GNF 7Bcr-AblAck1Activated Cdc42 kinase 1TNK2chronicmyelogenousleukemiaCMLAMLT315ImutationT315I-Bcr-AblInhibitorinhibitorinhibit

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GNF-7

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GNF-7 Related Antibodies

2 Publications Citing Use of MCE GNF-7

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Complete Stock Solution Preparation Table

GNF-7 Related Classifications

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