GNF-5

Modify Date: 2024-01-02 11:26:41

GNF-5 structure	Common Name	GNF-5
	CAS Number	778277-15-9	Molecular Weight	418.369
	Density	1.4±0.1 g/cm3	Boiling Point	612.4±55.0 °C at 760 mmHg
	Molecular Formula	C₂₀H₁₇F₃N₄O₃	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	324.2±31.5 °C
	Symbol	GHS06	Signal Word	Danger

Use of GNF-5

GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22±0.1 uM (Wild type Abl).IC50 Value: 0.22±0.1 uM (Wild type Abl) [1]Target: Abl GNF-5 is a cell-permeable GNF-2 N-hydroxyethyl carboxamide analog that exhibits in vivo efficacy in suppressing the proliferation of Bcr-abl-expressing Ba/F3 (93% and 83% of no-treatment control, respectively, on days 5 and 7 post treatment; 100 mg/kg b.i.d.) and bone marrow cells (~75% of no-treatment control in both WBC counts and spleen weight on day 7 post treatment; 50 mg/kg b.i.d.) in murine xenograft models of leukemia. Similar to GNF-2, GNF-5 exerts its effect via an allosteric mechanism (IC50 = 0.22 M against wild-type Abl) by targeting the myristate-binding pocket near the c-terminus of Abl kinase domain and thereby altering the conformational dynamics of the ATP-binding pocket. GNF-5 is ineffective toward the myristate-binding site mutant E505K and the ATP-binding site 'gatekeeper' mutant T315I.

Name	N-(2-hydroxyethyl)-3-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide
Synonym	More Synonyms

Description	GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22±0.1 uM (Wild type Abl).IC50 Value: 0.22±0.1 uM (Wild type Abl) [1]Target: Abl GNF-5 is a cell-permeable GNF-2 N-hydroxyethyl carboxamide analog that exhibits in vivo efficacy in suppressing the proliferation of Bcr-abl-expressing Ba/F3 (93% and 83% of no-treatment control, respectively, on days 5 and 7 post treatment; 100 mg/kg b.i.d.) and bone marrow cells (~75% of no-treatment control in both WBC counts and spleen weight on day 7 post treatment; 50 mg/kg b.i.d.) in murine xenograft models of leukemia. Similar to GNF-2, GNF-5 exerts its effect via an allosteric mechanism (IC50 = 0.22 M against wild-type Abl) by targeting the myristate-binding pocket near the c-terminus of Abl kinase domain and thereby altering the conformational dynamics of the ATP-binding pocket. GNF-5 is ineffective toward the myristate-binding site mutant E505K and the ATP-binding site 'gatekeeper' mutant T315I.
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl Research Areas >> Cancer
References	[1]. Zhang J, et al. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature. 2010 Jan 28;463(7280):501-6. [2]. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183.

Description

Related Catalog

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl

Research Areas >> Cancer

References

[1]. Zhang J, et al. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature. 2010 Jan 28;463(7280):501-6.

[2]. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183.

Density	1.4±0.1 g/cm3
Boiling Point	612.4±55.0 °C at 760 mmHg
Molecular Formula	C₂₀H₁₇F₃N₄O₃
Molecular Weight	418.369
Flash Point	324.2±31.5 °C
Exact Mass	418.125275
PSA	99.86000
LogP	3.31
Appearance of Characters	white to beige
Vapour Pressure	0.0±1.9 mmHg at 25°C
Index of Refraction	1.600
Storage condition	2-8°C
Water Solubility	DMSO: soluble10mg/mL (clear solution)

GNF-5 MSDS(Chinese)

Symbol	GHS06
Signal Word	Danger
Hazard Statements	H301-H319
Precautionary Statements	P301 + P310-P305 + P351 + P338
Hazard Codes	T
Risk Phrases	25-36
Safety Phrases	22-45
RIDADR	UN 2811 6.1 / PGIII
HS Code	2933599090

3-(6-((4-(trifl...

CAS#:714962-05-7

2-Aminoethanol

CAS#:141-43-5

~79%

GNF-5

CAS#:778277-15-9

Literature: Deng, Xianming; Okram, Barun; Ding, Qiang; Zhang, Jianming; Choi, Yongmun; Adrian, Francisco J.; Wojciechowski, Amy; Zhang, Guobao; Che, Jianwei; Bursulaya, Badry; Cowan-Jacob, Sandra W.; Rummel, Gabriele; Sim, Taebo; Gray, Nathanael S. Journal of Medicinal Chemistry, 2010 , vol. 53, # 19 p. 6934 - 6946

Precursor 2
CAS#:714962-05-7 3-(6-((4-(trifl... CAS#:141-43-5 2-Aminoethanol
DownStream 0

HS Code	2933599090
Summary	2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Benzamide,N-(2-hydroxyethyl)-3-(6-((4-(trifluoromethoxy)phenyl)amino)-4-pyrimidinyl)

QC-4300

Benzamide, N-(2-hydroxyethyl)-3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]-

N-(2-hydroxyethyl)-3-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzamide

GNF-5

N-(2-Hydroxyethyl)-3-(6-{[4-(trifluoromethoxy)phenyl]amino}-4-pyrimidinyl)benzamide

UNII-3ZUA56XMQQ

DC Chemicals Limited
China
Product Name: GNF-5
Price: $350.0/100mg $600.0/250mg $1500.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

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GNF-5

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