GNF-2 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide
GNF-2
CAS: 778270-11-4
Molecular Formula: C18H13F3N4O2
GNF-2 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide - Names and Identifiers
GNF-2 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide - Physico-chemical Properties
| Molecular Formula | C18H13F3N4O2 |
| Molar Mass | 374.32 |
| Solubility | Soluble in DMSO or EtOH |
| Appearance | White solid |
| Color | off-white |
| Storage Condition | 2-8°C |
| MDL | MFCD09265253 |
| Use | GNF-2 is a highly selective, non-ATP competitive Bcr-Abl inhibitor with no action activity against Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells. |
| In vitro study | 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 IC 50 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 IC 50 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 (IC 50 values of 268 and 194 nM, respectively). GNF-2 (1-10 μM; 48 hours) induces apoptosis of Bcr-abl-transformed cells. GNF-2 (0.1-10 μM; 90 minutes) inhibits the cellular tyrosine phosphorylation of Bcr-abl in a dose-dependent manner with an IC 50 of 267 nM. Cell Proliferation Assay 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 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 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 study | 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. GNF-2 prevents the LPS-induced increases of N.Oc/B.Pm, the percentage of Oc.S/BS, and the percentage of ES/BS. Animal Model: Eight-week-old C57/BL6 mice were administered i.p. injections of LPS (5 mg/kg) 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. |
GNF-2 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
GNF-2 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.672 ml | 13.358 ml | 26.715 ml |
| 5 mM | 0.534 ml | 2.672 ml | 5.343 ml |
| 10 mM | 0.267 ml | 1.336 ml | 2.672 ml |
| 5 mM | 0.053 ml | 0.267 ml | 0.534 ml |
Last Update：2024-01-02 23:10:35
GNF-2 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide - Reference Information
| biological activity | GNF-2 is a highly selective, allosteric, non-ATP competitive Bcr-Abl inhibitor. GNF-2 inhibition of Ba/F3.p210 proliferation, IC50 138 nM. |
| Target | Bcr-Abl |
| in vitro study | GNF-2 selective indications Bcr-abl-dependent cell propagation. GNF-2 (0.005-10 μm; 48 hours) specifically inhibit the propagation of the Bcr-abl-expressing cells with an IC 50 of 138 nM and not show any cyanographic 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 IC 50 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 (IC 50 values of 268 and 194 nM, respectively). GNF-2 (1-10 μM; 48 hours) induces apoptosis of Bcr-abl-transformed cells. GNF-2 (0.1-10 μM; 90 minutes) inhibits the cellular tyrosine phosphorylation of Bcr-abl in a dose-dependent manner with an IC 50 of 267 nM. Cell Proliferation Assay 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 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 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. |
| Cell Line: | Ba/F3.p210, Ba/F3.p210 E255V and Ba/F3.p185 Y253H cells Ba/F3.p210 and Ba/F3.p210 E255V cells Ba/F3.p210 and Ba/F3.p210 E255V cells |
| Concentration: | 0.005, 0.01, 0.1, 1, 10 μM 1, 10 μM 0.1, 1, 10 μM |
| Incubation Time: | 48 hours 48 hours 90 minutes |
| Result: | Inhibited Bcr-abl-transformed cells proliferation. 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. 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. Prevented inflammatory bone destruction in vivo. |
| in vivo studies | oer-2 (10 mg/kg; I. p. for 8 days) protectts LPS (5 mg/kg) induced bone erosion in mice. GNF-2 protects the LPS induced bone loss and abrogates the LPS-induced amounts of bone volume/tissue volume (BV/TV) of LPS-treated mice. GNF-2 prevent the LPS-induced increases of N.Oc/B.Pm, the percentage of Oc.S/BS, and the percentage of ES/BS. Animal Model: Eight-week-old C57/BL6 mice were administered I .p. injections of LPS (5 mg/kg) 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. |
| Animal Model: | Eight-week-old C57/BL6 mice were administered i.p. injections of LPS (5 mg/kg) |
| Dosage: | 10 mg/kg |
| Administration: | I.p. injections for 8 days; 1 day before and every day after the LPS injection |
Last Update：2024-04-10 22:29:15
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Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
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WhatsApp: +86-18621343501
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Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
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View History
GNF-2 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide
Cbz-1-Amino-1-Cyclopentanecarboxylic Acid
CHROMIC NITRATE NONAHYDRATE
DI-POTASSIUM HYDROGEN ORTHOPHOSPHATE 3-HYDRATE
6,13-BIS(TRIISOPROPYLSILYLETHYNYL)PENTACENE6,13-BIS(TRIISOPROPYLSILYLETHYNYL)PENTACENE6,13-BIS(TRIISOPROPYLSILYLETHYNYL)PENTACENE
PYROGLU-GLY-PRO-TRP-LEU-GLU-GLU-GLU-GLU-GLU-ALA-TYR-GLY-TRP-MET-ASP-PHE-NH2
(E)3-[(4-T-BUTYLPHENYL)SULFONYL]-2-PROPENENITRILE
DIMETHYLPHENACYLSULPHONIUM TETRAFLUOROBORATE
Anti-CSF 140 kDa subunit
yttrium tripropan-2-olate
Cbz-1-Amino-1-Cyclopentanecarboxylic Acid
CHROMIC NITRATE NONAHYDRATE
DI-POTASSIUM HYDROGEN ORTHOPHOSPHATE 3-HYDRATE
6,13-BIS(TRIISOPROPYLSILYLETHYNYL)PENTACENE6,13-BIS(TRIISOPROPYLSILYLETHYNYL)PENTACENE6,13-BIS(TRIISOPROPYLSILYLETHYNYL)PENTACENE
PYROGLU-GLY-PRO-TRP-LEU-GLU-GLU-GLU-GLU-GLU-ALA-TYR-GLY-TRP-MET-ASP-PHE-NH2
(E)3-[(4-T-BUTYLPHENYL)SULFONYL]-2-PROPENENITRILE
DIMETHYLPHENACYLSULPHONIUM TETRAFLUOROBORATE
Anti-CSF 140 kDa subunit
yttrium tripropan-2-olate