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GNF-2 structure, CAS 778270-11-4

GNF-2

CAS Number778270-11-4

Synonyms3k5v; 3-(6-{[4-(Trifluoromethoxy)phenyl]amino}-4-pyrimidinyl)benzamide; GNF-2

Molecular FormulaC18H13F3N4O2

Molecular Weight374.317

Purity

Density1.4±0.1 g/cm3

Boiling Point536.4±50.0 °C at 760 mmHg

Melting Point

Flash Point

Appearanceoff-white

EINECS

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Cat. No.: 2A-1198798 Purity:
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Quality Control of [ 778270-11-4 ] SDS Specification MoL

COA NMR CNMR HPLC LC-MS
Chemical & Physical Properties
CAS Number778270-11-4
Catalog No.2A-1198798
Chinese Name3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺
Synonyms3k5v; 3-(6-{[4-(Trifluoromethoxy)phenyl]amino}-4-pyrimidinyl)benzamide; GNF-2
Molecular FormulaC18H13F3N4O2
Molecular Weight374.317
Density1.4±0.1 g/cm3
Boiling Point536.4±50.0 °C at 760 mmHg
Appearanceoff-white
Water SolubilityH2O: <2mg/mL
Storage Condition2-8°C
ApplicationGNF-2 is a non-ATP competitive Bcr-Abl selective inhibitor with an IC50 of 140nM.
SMILESNC(=O)c1cccc(-c2cc(Nc3ccc(OC(F)(F)F)cc3)ncn2)c1
InChI KeyWEVYNIUIFUYDGI-UHFFFAOYSA-N
Hazard Symbolstransportation
MSDSmsds/200740_2_778270_11_4.pdf
BioactivityGNF-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]. Related Catalog Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl Research Areas >> Cancer References [1]. Adrián FJ, et al. Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol. 2006 Feb;2(2):95-102. [2]. Khateb M, et al. Overcoming Bcr-Abl T315I mutation by combination of GNF-2 and ATP competitors in an Abl-independent mechanism. BMC Cancer. 2012 Nov 27;12:563. [3]. Mian AA, et al. Allosteric inhibition enhances the efficacy of ABL kinase inhibitors to target unmutated BCR-ABL and BCR-ABL-T315I.BMC Cancer. 2012 Sep 17;12:411. [4]. Kim HJ, et al. The tyrosine kinase inhibitor GNF-2 suppresses osteoclast formation and activity. J Leukoc Biol. 2013 Oct 15. [5]. Huang WC, et al. Glucosylceramide synthase inhibitor PDMP sensitizes chronic myeloid leukemia T315I mutant to Bcr-Abl inhibitor and cooperatively induces glycogen synthase kinase-3-regulated apoptosis. FASEB J. 2011 Oct;25(10):3661-73. Chemical & Physical Properties 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 InChIKey WEVYNIUIFUYDGI-UHFFFAOYSA-N SMILES NC(=O)c1cccc(-c2cc(Nc3ccc(OC(F)(F)F)cc3)ncn2)c1 Storage condition 2-8°C Water Solubility H2O: <2mg/mL
Use ofProperties Name 3-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide Synonym More Synonyms GNF-2 Biological Activity Related Catalog Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl Research Areas >> Cancer References [1]. Adrián FJ, et al. Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol. 2006 Feb;2(2):95-102. [2]. Khateb M, et al. Overcoming Bcr-Abl T315I mutation by combination of GNF-2 and ATP competitors in an Abl-independent mechanism. BMC Cancer. 2012 Nov 27;12:563. [3]. Mian AA, et al. Allosteric inhibition enhances the efficacy of ABL kinase inhibitors to target unmutated BCR-ABL and BCR-ABL-T315I.BMC Cancer. 2012 Sep 17;12:411. [4]. Kim HJ, et al. The tyrosine kinase inhibitor GNF-2 suppresses osteoclast formation and activity. J Leukoc Biol. 2013 Oct 15. [5]. Huang WC, et al. Glucosylceramide synthase inhibitor PDMP sensitizes chronic myeloid leukemia T315I mutant to Bcr-Abl inhibitor and cooperatively induces glycogen synthase kinase-3-regulated apoptosis. FASEB J. 2011 Oct;25(10):3661-73. Chemical & Physical Properties Molecular Formula C18H13F3N4O2 Exact Mass 374.099060 PSA 90.13000 Appearance of Characters off-white Index of Refraction 1.611 InChIKey WEVYNIUIFUYDGI-UHFFFAOYSA-N
Transport InfoProduct name: Purity: 98.0%
MSDS Transport InfoModule 14. Shipping information 14.1 UN number European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.2 Names specified by the United Nations (UN) European Land Transport Dangerous Regulations: No dangerous goods IMDG Code: No dangerous goods International Air Transport Dangerous Regulations: No dangerous goods 14.3 Transport hazard categories European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.4 Package group European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.5 Environmental hazards European Land Transport Dangerous Regulations: No International Maritime Transport Dangerous Regulations Maritime Pollutants: No International Air Transport Risk Regulations: No 14.6 Special precautions for users No data available
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