GNF-7
Based on 2 publication(s) in Google Scholar
GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-AblWT and Bcr-AblT315I, 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.
- Purity: 99.70%
- CAS No.: 839706-07-9
- Formula: C28H24F3N7O2
- Molecular Weight:547.53
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) GNF-7
More
Biological Activity
IC50: 133 nM (Bcr-AblWT)[1], 61 nM (Bcr-AblT315I)[1], 25 nM (ACK1)[3], 8 nM (GCK)[3]
|
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: 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 |
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 |
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 |
<5 nM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant
|
[PMID: 20604564] |
| BaF3 | IC50 |
<5 nM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant
|
[PMID: 20604564] |
| BaF3 | IC50 |
<5 nM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F317L mutant
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F317L mutant
|
[PMID: 20604564] |
| BaF3 | IC50 |
<5 nM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant
|
[PMID: 20604564] |
| BaF3 | IC50 |
<5 nM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant
|
[PMID: 20604564] |
| BaF3 | IC50 |
<5 nM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant
|
[PMID: 20604564] |
| BaF3 | IC50 |
<5 nM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant
|
[PMID: 20604564] |
| BaF3 | IC50 |
<5 nM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl
Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl
|
[PMID: 20604564] |
| BaF3 | IC50 |
0.008 μM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing TrkC
Antiproliferative activity against mouse BA/F3 cells expressing TrkC
|
[PMID: 20604564] |
| BaF3 | IC50 |
0.009 μM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing FGFR3
Antiproliferative activity against mouse BA/F3 cells expressing FGFR3
|
[PMID: 20604564] |
| BaF3 | IC50 |
0.011 μM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing PDGFR
Antiproliferative activity against mouse BA/F3 cells expressing PDGFR
|
[PMID: 20604564] |
| BaF3 | IC50 |
0.012 μM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing Flt3-ITD
Antiproliferative activity against mouse BA/F3 cells expressing Flt3-ITD
|
[PMID: 20604564] |
| BaF3 | IC50 |
0.044 μM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing JAK1
Antiproliferative activity against mouse BA/F3 cells expressing JAK1
|
[PMID: 20604564] |
| BaF3 | IC50 |
0.05 μM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing JAK2 V617F mutant
Antiproliferative activity against mouse BA/F3 cells expressing JAK2 V617F mutant
|
[PMID: 20604564] |
| BaF3 | IC50 |
0.127 μM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing JAK2
Antiproliferative activity against mouse BA/F3 cells expressing JAK2
|
[PMID: 20604564] |
| BaF3 | IC50 |
0.359 μM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing Flt3
Antiproliferative activity against mouse BA/F3 cells expressing Flt3
|
[PMID: 20604564] |
| BaF3 | IC50 |
1.466 μM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing NPM-ALK
Antiproliferative activity against mouse BA/F3 cells expressing NPM-ALK
|
[PMID: 20604564] |
| BaF3 | IC50 |
11 nM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant
|
[PMID: 20604564] |
| BaF3 | IC50 |
1370 nM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells
Antiproliferative activity against mouse BA/F3 cells
|
[PMID: 20604564] |
| BaF3 | IC50 |
2.018 μM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing JAK3
Antiproliferative activity against mouse BA/F3 cells expressing JAK3
|
[PMID: 20604564] |
| 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 |
3.401 μM
Compound: 2, GNF-7
|
Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met
Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met
|
[PMID: 20604564] |
| 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] |
| COLO 205 | IC50 |
0.005 μM
Compound: 2, GNF-7
|
Antiproliferative activity against human COLO205 cells
Antiproliferative activity against human COLO205 cells
|
[PMID: 20604564] |
| HEK-293T | IC50 |
>10 μM
Compound: 2, GNF-7
|
Antiproliferative activity against human HEK293T cells
Antiproliferative activity against human HEK293T cells
|
[PMID: 20604564] |
| 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] |
| HT-29 | EC50 |
100 nM
Compound: GNF-7; L4
|
Anti-necroptosis activity against TSZ-induced human HT-29 cells
Anti-necroptosis activity against TSZ-induced human HT-29 cells
|
[PMID: 38199165] |
| 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] |
| SW-620 | IC50 |
0.001 μM
Compound: 2, GNF-7
|
Antiproliferative activity against human SW620 cells
Antiproliferative activity against human SW620 cells
|
[PMID: 20604564] |
| U-87MG ATCC | IC50 |
5.956 μM
Compound: 2, GNF-7
|
Antiproliferative activity against human U87 cells
Antiproliferative activity against human U87 cells
|
[PMID: 20604564] |
| 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] |
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.
-
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.
-
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 Line:OCI-AML3 cells
-
Concentration:1 μM
-
Incubation Time:24 hours
-
Result:Induced of G0-G1 arrest.
GNF-7 exhibits moderate oral bioavailability (mice 36%) and Cmax (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%), Cmax (3616 nM), T1/2 (3.2 h).
Chemical Information
-
CAS No. 839706-07-9
-
Appearance Solid
-
Molecular Weight 547.53
-
Formula C28H24F3N7O2
-
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
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
Biochem Pharmacol
The Bcr-Abl inhibitor GNF-7 inhibits necroptosis and ameliorates acute kidney injury by targeting RIPK1 and RIPK3 kinases. [Abstract]2020 Jul;177:113947. PMID: 32247850 -
Arch Pharm (Weinheim)
Discovery of potent CSK inhibitors through integrated virtual screening and molecular dynamic simulation. [Abstract]2024 Sep;357(9):e2400066. PMID: 38809025
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
-
Data Sheet (277 KB)
-
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Portuguese - PT (480 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
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.
| 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 |