GNF-2
Modify Date: 2024-01-02 17:12:50
GNF-2 structure
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Common Name | GNF-2 | ||
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| CAS Number | 778270-11-4 | Molecular Weight | 374.317 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 536.4±50.0 °C at 760 mmHg | |
| Molecular Formula | C18H13F3N4O2 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 278.2±30.1 °C | |
| Symbol |
GHS07 |
Signal Word | Warning | |
Use of GNF-2GNF-2 is a highly selective non-ATP competitive inhibitor of oncogenic Bcr-Abl activity (IC50 = 0.14 μM).IC50 value: 0.14 uM [1]Target: Bcr-Ablin vitro: Ba/F3 cells harboring native or T315I mutated Bcr-Abl constructs were treated with GNF-2 and AKIs. We monitored the effect of GNF-2 with AKIs on the proliferation and clonigenicity of the different Ba/F3 cells. In addition, we monitored the auto-phosphorylation activity of Bcr-Abl and JAK2 in cells treated with GNF-2 and AKIs [2]. GNF-2 increased the effects of AKIs on unmutated BCR/ABL. Interestingly, the combination of Dasatinib and GNF-2 overcame resistance of BCR/ABL-T315I in all models used in a synergistic manner [3].GNF-2 dose-dependently inhibited the proliferation of osteoclast precursors through the suppression of the M-CSFR c-Fms. In addition, GNF-2 accelerated osteoclast apoptosis by inducing caspase-3 and Bim expression. Furthermore, GNF-2 interfered with actin cytoskeletal organization and subsequently blocked the bone-resorbing activity of mature osteoclasts [4].in vivo: Combining PDMP and GNF-2 eliminated transplanted-CML-T315I-mutants in vivo and dose dependently sensitized primary cells from CML T315I patients to GNF-2-induced proliferation inhibition and apoptosis[5]. |
| Name | 3-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide |
|---|---|
| Synonym | More Synonyms |
| Description | GNF-2 is a highly selective non-ATP competitive inhibitor of oncogenic Bcr-Abl activity (IC50 = 0.14 μM).IC50 value: 0.14 uM [1]Target: Bcr-Ablin vitro: Ba/F3 cells harboring native or T315I mutated Bcr-Abl constructs were treated with GNF-2 and AKIs. We monitored the effect of GNF-2 with AKIs on the proliferation and clonigenicity of the different Ba/F3 cells. In addition, we monitored the auto-phosphorylation activity of Bcr-Abl and JAK2 in cells treated with GNF-2 and AKIs [2]. GNF-2 increased the effects of AKIs on unmutated BCR/ABL. Interestingly, the combination of Dasatinib and GNF-2 overcame resistance of BCR/ABL-T315I in all models used in a synergistic manner [3].GNF-2 dose-dependently inhibited the proliferation of osteoclast precursors through the suppression of the M-CSFR c-Fms. In addition, GNF-2 accelerated osteoclast apoptosis by inducing caspase-3 and Bim expression. Furthermore, GNF-2 interfered with actin cytoskeletal organization and subsequently blocked the bone-resorbing activity of mature osteoclasts [4].in vivo: Combining PDMP and GNF-2 eliminated transplanted-CML-T315I-mutants in vivo and dose dependently sensitized primary cells from CML T315I patients to GNF-2-induced proliferation inhibition and apoptosis[5]. |
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| Related Catalog | |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 536.4±50.0 °C at 760 mmHg |
| Molecular Formula | C18H13F3N4O2 |
| Molecular Weight | 374.317 |
| Flash Point | 278.2±30.1 °C |
| Exact Mass | 374.099060 |
| PSA | 90.13000 |
| LogP | 3.68 |
| Appearance of Characters | off-white |
| Vapour Pressure | 0.0±1.4 mmHg at 25°C |
| Index of Refraction | 1.611 |
| Storage condition | 2-8°C |
| Water Solubility | H2O: <2mg/mL |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H315-H319-H335 |
| Precautionary Statements | P261-P305 + P351 + P338 |
| Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Gloves |
| Hazard Codes | Xi |
| Risk Phrases | 36/37/38 |
| Safety Phrases | 26 |
| RIDADR | NONH for all modes of transport |
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GNF-2 CAS#:778270-11-4 |
| Literature: Journal of the American Chemical Society, , vol. 134, # 22 p. 9138 - 9141 |
| Precursor 1 | |
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| DownStream 0 | |
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Allosteric inhibitors of Bcr-abl-dependent cell proliferation.
Nat. Chem. Biol. 2 , 95-102, (2006) Chronic myelogenous leukemia (CML) is a myeloproliferative disorder characterized at the molecular level by the expression of Bcr-abl, a 210-kDa fusion protein with deregulated tyrosine kinase activit... |
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Inhibitors of Bcr-abl... breaking new ground again.
Nat. Chem. Biol. 2nd ed.,, 63-64, (2006)
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| Benzamide, 3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]- |
| 3k5v |
| 3-(6-{[4-(Trifluoromethoxy)phenyl]amino}-4-pyrimidinyl)benzamide |
| GNF-2 |
| Bcr-abl Inhibitor |