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

MedKoo Cat#: 407257 | Name: GNF-7

Description:

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

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

Theoretical Analysis

MedKoo Cat#: 407257

Name: GNF-7

CAS#: 839706-07-9

Chemical Formula: C28H24F3N7O2

Exact Mass: 547.1944

Molecular Weight: 547.54

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 650.00	2 Weeks
100mg	USD 1,150.00	2 Weeks
200mg	USD 1,850.00	2 Weeks
500mg	USD 2,750.00	2 Weeks
1g	USD 3,450.00	2 Weeks

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Related CAS #

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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

View handling instruction

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

	Solvent	mg/mL	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

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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:

In vivo protocol:

TBD

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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Penoxsulam

MedKoo CAT#: 126282

CAS#: 219714-96-2