GNF-5 free base · Synonyms: GNF 5 · GNF5

GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor.

For research use only. Not for human or veterinary use.

Target Bcr-Abl

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

GNF-5 structure

CAS No.: 778277-15-9

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 620.00	BP-02121-500mg	In stock	Get quote
1 g	USD 980.00	BP-02121-1g	In stock	Get quote
2 g	USD 1,560.00	BP-02121-2g	In stock	Get quote
5 g	USD 3,000.00	BP-02121-5g	In stock	Get quote

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Description

GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC50 value of 0.22 µM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer .

Biological activity

In Vitro GNF-5 has inhibition of wild-type Abl with an IC50 value of 0.22 µM but no inhibition for myristate site mutant E505K (IC50 ＞10 µM). In Vivo GNF-5 (5 mg/kg iv. or 20 mg/kg oral) has suitable pharmacokinetic parameters. GNF-5 (oral, 50 or 100 mg/kg, twice daily, for 7 days) shows efficacious in vivo but can observe relapses. GNF-5 (75 mg/kg, b.i.d) inhibits T315I Bcr-Abl combination with nilotinib in vivo.

Identifiers

SMILES: OCCNC(=O)C1=CC=CC(=C1)C1=NC=NC(NC2=CC=C(OC(F)(F)F)C=C2)=C1
InChIKey: IIQUYGWWHIHOCF-UHFFFAOYSA-N

Specifications

MW (average): 418.3692
Formula: C₂₀H₁₇F₃N₄O₃
CAS No.: 778277-15-9
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; 4℃ 2 years; In solvent -20℃ 1 year;

Solubility

Soluble in DMSO

Documents

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.

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