GNF-7 | CAS#839706-07-9 | type-II T315I inhibitor

GNF-7
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407257

CAS#: 839706-07-9

Description: GNF-7 is a type-II T315I inhibitor. GNF-7 inhibits Ack1 and germinal center kinase (GCK). GNF-7 displayed significant in vivo efficacy against T315I-Bcr-Abl without appreciable toxicity in a bioluminescent xenograft mouse model using a transformed T315I-Bcr-Abl-Ba/F3 cell line that has a stable luciferase expression. GNF-7 is among the first type-II inhibitors capable of inhibiting T315I to be described and will serve as a valuable lead to design the third generation Bcr-Abl kinase inhibitors.

Chemical Structure

GNF-7

CAS# 839706-07-9

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 407257
Name: GNF-7
CAS#: 839706-07-9
Chemical Formula: C28H24F3N7O2
Exact Mass: 547.19
Molecular Weight: 547.542
Elemental Analysis: C, 61.42; H, 4.42; F, 10.41; N, 17.91; O, 5.84

Price and Availability

Size	Price	Availability
50mg	USD 650	2 Weeks
100mg	USD 1150
200mg	USD 1850
500mg	USD 2750
1g	USD 3450
2g	USD 5450
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: GNF-7; GNF7; GNF 7.

IUPAC/Chemical Name: N-(4-methyl-3-(1-methyl-7-((6-methylpyridin-3-yl)amino)-2-oxo-1,4-dihydropyrimido[4,5-d]pyrimidin-3(2H)-yl)phenyl)-3-(trifluoromethyl)benzamide

InChi Key: SZNYUUZOQHNEKB-UHFFFAOYSA-N

InChi Code: InChI=1S/C28H24F3N7O2/c1-16-7-9-21(34-25(39)18-5-4-6-20(11-18)28(29,30)31)12-23(16)38-15-19-13-33-26(36-24(19)37(3)27(38)40)35-22-10-8-17(2)32-14-22/h4-14H,15H2,1-3H3,(H,34,39)(H,33,35,36)

SMILES Code: O=C(NC1=CC=C(C)C(N2CC3=CN=C(NC4=CC=C(C)N=C4)N=C3N(C)C2=O)=C1)C5=CC=CC(C(F)(F)F)=C5

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

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively.
In vitro activity:	GNF-7 effectively suppressed proliferation of cancer cells harboring mtRAS with submicromolar potencies (GI50s = 0.169 to 0.938 µM). Reference: Front Oncol. 2021 Dec 9;11:768022. https://pubmed.ncbi.nlm.nih.gov/34956887/
In vivo activity:	TBD

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	10.0	18.26
	DMF:PBS (pH 7.2) (1:2)	0.3	0.55
	DMSO	20.6	37.61
	Ethanol	0.1	0.18

Preparing Stock Solutions

The following data is based on the product molecular weight 547.54 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.

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

Formulation protocol:	1. Kim N, Shin I, Kim Y, Jeon E, Lee J, Lee C, Nam Y, Lee S, Ju E, Kim C, Son W, Ryu S, Ko M, Sim T. Novel Small Molecules Capable of Blocking mtRAS-Signaling Pathway. Front Oncol. 2021 Dec 9;11:768022. doi: 10.3389/fonc.2021.768022. PMID: 34956887; PMCID: PMC8695447.
In vitro protocol:	1. Kim N, Shin I, Kim Y, Jeon E, Lee J, Lee C, Nam Y, Lee S, Ju E, Kim C, Son W, Ryu S, Ko M, Sim T. Novel Small Molecules Capable of Blocking mtRAS-Signaling Pathway. Front Oncol. 2021 Dec 9;11:768022. doi: 10.3389/fonc.2021.768022. PMID: 34956887; PMCID: PMC8695447.
In vivo protocol:	TBD

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1: Liang X, Liu X, Wang B, Zou F, Wang A, Qi S, Chen C, Zhao Z, Wang W, Qi Z, Lv
F, Hu Z, Wang L, Zhang S, Liu Q, Liu J. Discovery of
2-((3-amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phe
nyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a potent,
selective and orally available BCR-ABL/SRC/p38 kinase inhibitor for Chronic
Myeloid Leukemia. J Med Chem. 2016 Jan 20. [Epub ahead of print] PubMed PMID:
26789553.

2: Lu X, Zhang Z, Ren X, Pan X, Wang D, Zhuang X, Luo J, Yu R, Ding K. Hybrid
pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I)
mutant. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3458-63. doi:
10.1016/j.bmcl.2015.07.006. Epub 2015 Jul 9. PubMed PMID: 26195136.

3: Nonami A, Sattler M, Weisberg E, Liu Q, Zhang J, Patricelli MP, Christie AL,
Saur AM, Kohl NE, Kung AL, Yoon H, Sim T, Gray NS, Griffin JD. Identification of
novel therapeutic targets in acute leukemias with NRAS mutations using a
pharmacologic approach. Blood. 2015 May 14;125(20):3133-43. doi:
10.1182/blood-2014-12-615906. Epub 2015 Apr 1. PubMed PMID: 25833960; PubMed
Central PMCID: PMC4432008.

4: Choi HG, Ren P, Adrian F, Sun F, Lee HS, Wang X, Ding Q, Zhang G, Xie Y, Zhang
J, Liu Y, Tuntland T, Warmuth M, Manley PW, Mestan J, Gray NS, Sim T. A type-II
kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl.
J Med Chem. 2010 Aug 12;53(15):5439-48. doi: 10.1021/jm901808w. PubMed PMID:
20604564; PubMed Central PMCID: PMC4134510.

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