GNF-5
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MedKoo CAT#: 407206

CAS#: 778277-15-9

Description: GNF-5 is a selective allosteric inhibitor of Bcr-Abl (IC50 = 220 nM for wild-type Abl). GNF-5 has improved pharmacokinetic properties, when used in combination with the ATP-competitive inhibitors imatinib or nilotinib, suppressed the emergence of resistance mutations in vitro, displayed additive inhibitory activity in biochemical and cellular assays against T315I mutant human Bcr-Abl and displayed in vivo efficacy against this recalcitrant mutant in a murine bone-marrow transplantation model.


Chemical Structure

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GNF-5
CAS# 778277-15-9

Theoretical Analysis

MedKoo Cat#: 407206
Name: GNF-5
CAS#: 778277-15-9
Chemical Formula: C20H17F3N4O3
Exact Mass: 418.12528
Molecular Weight: 418.37621
Elemental Analysis: C, 57.42; H, 4.10; F, 13.62; N, 13.39; O, 11.47

Price and Availability

Size Price Availability Quantity
25.0mg USD 110.0 Same day
50.0mg USD 190.0 Same day
100.0mg USD 350.0 Same day
200.0mg USD 630.0 Same day
500.0mg USD 1350.0 Same day
1.0g USD 2430.0 2 weeks
2.0g USD 4250.0 2 weeks
5.0g USD 6450.0 2 weeks
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Synonym: GNF-5; GNF 5; GNF5.

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

InChi Key: IIQUYGWWHIHOCF-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H17F3N4O3/c21-20(22,23)30-16-6-4-15(5-7-16)27-18-11-17(25-12-26-18)13-2-1-3-14(10-13)19(29)24-8-9-28/h1-7,10-12,28H,8-9H2,(H,24,29)(H,25,26,27)

SMILES Code: O=C(NCCO)C1=CC=CC(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)=C1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: 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 Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 418.37621 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Skora L, Kempf D, Mestan J, D'Orazio D, Jahnke W. Phosphorylation of Tyr245 in the open-inhibited state of Abelson kinase does not induce downstream signaling. Eur J Haematol. 2015 Jul 7. doi: 10.1111/ejh.12627. [Epub ahead of print] PubMed PMID: 26154982.

2: Karunakaran U, Park SJ, Jun do Y, Sim T, Park KG, Kim MO, Lee IK. Non-receptor tyrosine kinase inhibitors enhances β-cell survival by suppressing the PKCδ signal transduction pathway in streptozotocin-induced β-cell apoptosis. Cell Signal. 2015 Jun;27(6):1066-74. doi: 10.1016/j.cellsig.2015.01.018. Epub 2015 Feb 12. PubMed PMID: 25683919.

3: Chen S, Tang DD. c-Abl tyrosine kinase regulates cytokinesis of human airway smooth muscle cells. Am J Respir Cell Mol Biol. 2014 Jun;50(6):1076-83. doi: 10.1165/rcmb.2013-0438OC. PubMed PMID: 24392933; PubMed Central PMCID: PMC4068917.

4: Skora L, Mestan J, Fabbro D, Jahnke W, Grzesiek S. NMR reveals the allosteric opening and closing of Abelson tyrosine kinase by ATP-site and myristoyl pocket inhibitors. Proc Natl Acad Sci U S A. 2013 Nov 19;110(47):E4437-45. doi: 10.1073/pnas.1314712110. Epub 2013 Nov 4. PubMed PMID: 24191057; PubMed Central PMCID: PMC3839726.

5: Cleary RA, Wang R, Wang T, Tang DD. Role of Abl in airway hyperresponsiveness and airway remodeling. Respir Res. 2013 Oct 11;14:105. doi: 10.1186/1465-9921-14-105. PubMed PMID: 24112389; PubMed Central PMCID: PMC3852349.

6: Iacob RE, Zhang J, Gray NS, Engen JR. Allosteric interactions between the myristate- and ATP-site of the Abl kinase. PLoS One. 2011 Jan 10;6(1):e15929. doi: 10.1371/journal.pone.0015929. PubMed PMID: 21264348; PubMed Central PMCID: PMC3018526.

7: Kim DH, Sim T. Chemical kinomics: a powerful strategy for target deconvolution. BMB Rep. 2010 Nov;43(11):711-9. doi: 10.5483/BMBRep.2010.43.11.711. Review. PubMed PMID: 21110913.

8: Deng X, Okram B, Ding Q, Zhang J, Choi Y, Adrián FJ, Wojciechowski A, Zhang G, Che J, Bursulaya B, Cowan-Jacob SW, Rummel G, Sim T, Gray NS. Expanding the diversity of allosteric bcr-abl inhibitors. J Med Chem. 2010 Oct 14;53(19):6934-46. doi: 10.1021/jm100555f. PubMed PMID: 20828158; PubMed Central PMCID: PMC2951064.

9: Zhang J, Adrián FJ, Jahnke W, Cowan-Jacob SW, Li AG, Iacob RE, Sim T, Powers J, Dierks C, Sun F, Guo GR, Ding Q, Okram B, Choi Y, Wojciechowski A, Deng X, Liu G, Fendrich G, Strauss A, Vajpai N, Grzesiek S, Tuntland T, Liu Y, Bursulaya B, Azam M, Manley PW, Engen JR, Daley GQ, Warmuth M, Gray NS. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature. 2010 Jan 28;463(7280):501-6. doi: 10.1038/nature08675. Epub 2010 Jan 13. PubMed PMID: 20072125; PubMed Central PMCID: PMC2901986.

GNF-5

25.0mg / USD 110.0