country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-160478

Copy Link Print Information

GNF-6

GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC₅₀s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation.

For research use only. We do not sell to patients.

CAS No.: 839708-29-1
Formula: C₂₂H₁₉F₃N₆O₂
Molecular Weight:456.42

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (265 KB)

GNF-6 Chemical Structure

CAS No.: 839708-29-1

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Bcr-Abl Isoforms :

Abl
Bcr-Abl

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	2.114 μM Compound: 10k	Growth inhibition of parental mouse BA/F3 cells after 72 hrs by celltiter-glo assay Growth inhibition of parental mouse BA/F3 cells after 72 hrs by celltiter-glo assay	[PMID: 30153003]
BaF3	IC₅₀	<5 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant	[PMID: 20604564]
BaF3	IC₅₀	<5 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant	[PMID: 20604564]
BaF3	IC₅₀	<5 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F317L mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F317L mutant	[PMID: 20604564]
BaF3	IC₅₀	<5 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant	[PMID: 20604564]
BaF3	IC₅₀	<5 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant	[PMID: 20604564]
BaF3	IC₅₀	<5 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant	[PMID: 20604564]
BaF3	IC₅₀	<5 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl	[PMID: 20604564]
BaF3	IC₅₀	1799 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells Antiproliferative activity against mouse BA/F3 cells	[PMID: 20604564]
BaF3	IC₅₀	243 nM Compound: 1, GNF-6	Inhibition of Bcr-Abl T315I mutant autophosphorylation in mouse BA/F3 cells Inhibition of Bcr-Abl T315I mutant autophosphorylation in mouse BA/F3 cells	[PMID: 20604564]
BaF3	IC₅₀	294 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant	[PMID: 20604564]
BaF3	IC₅₀	303 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant	[PMID: 20604564]
OCI-AML-3	GI₅₀	0.466 μM Compound: 10k	Growth inhibition of human OCI-AML3 cells harboring NRAS-Q61L mutant after 72 hrs by celltiter-glo assay Growth inhibition of human OCI-AML3 cells harboring NRAS-Q61L mutant after 72 hrs by celltiter-glo assay	[PMID: 30153003]
U-937	GI₅₀	4.967 μM Compound: 10k	Growth inhibition of parental human U937 cells after 72 hrs by celltiter-glo assay Growth inhibition of parental human U937 cells after 72 hrs by celltiter-glo assay	[PMID: 30153003]

Chemical Information

CAS No. 839708-29-1
Molecular Weight 456.42
Formula C₂₂H₁₉F₃N₆O₂
SMILES

O=C(C1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(C)C(N3C(N(C)C4=NC(N)=NC=C4C3)=O)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Protocols

All Animals and Diseases

Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (265 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. David F. Woodward, et al. Non-acidic cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl derivatives as therapeutic agents. WO1994006433A1. [Content Brief]

Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote