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Tocris/GNF 5/4908/10/10 mg

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货号: 4908/10

品牌: Tocris

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Description: Selective allosteric inhibitor of Bcr-Abl; analog of GNF 2 (Cat. No. 4399)

Chemical Name: N-(2-Hydroxyethyl)-3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Selective, non-ATP competitive allosteric inhibitor of Bcr-Abl (IC₅₀ = 220 nM for wild-type Abl). Binds the myristate-binding site of Abl. Acts in combination with nilotinib to inhibit T315I Bcr-Abl in vitro and in vivo. Analog of GNF 2 (Cat. No. 4399).

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GNF 5 is reviewed on the chemical probes website.

Compound Libraries

GNF 5 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	418.37
Formula	C₂₀H₁₇F₃N₄O₃
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	778277-15-9
PubChem ID	44129660
InChI Key	IIQUYGWWHIHOCF-UHFFFAOYSA-N
Smiles	O=C(NCCO)C1=CC(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)=CC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	41.84	100

Preparing Stock Solutions

The following data is based on the product molecular weight 418.37. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.39 mL	11.95 mL	23.9 mL
5 mM	0.48 mL	2.39 mL	4.78 mL
10 mM	0.24 mL	1.2 mL	2.39 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Zhang et al (2010) Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature 463 501 PMID: 20072125

Iacob et al (2011) Allosteric interactions between the myristate- and ATP-site of the Abl kinase. PLoS One 6 e15929 PMID: 21264348

Deng et al (2010) Expanding the diversity of allosteric Bcr-Abl inhibitors. J.Med.Chem. 53 6934 PMID: 20828158

Keywords: GNF 5, supplier, GNF5, Bcr-Abl, kinase, allosteric, inhbitors, inhibits, selective, bcrabl, bcr, abl, fusion, philadelphia, chromosome, chronic, myeloid, leukemia, leukaemia, CML, allosteric, Abl, Kinase, Abl, Kinase, Tocris Bioscience

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