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Art. -Nr.: HY-160478

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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.

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CAS. Nr.: 839708-29-1
Formel: C₂₂H₁₉F₃N₆O₂
Molecular Weight:456.42

Speicherung:

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

Data Sheet (265 KB)

GNF-6 Chemical Structure

CAS. Nr.: 839708-29-1

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Biologische Aktivität
- Beschreibung
- Cellular Effect
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen :

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. Nr. 839708-29-1
Molecular Weight 456.42
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 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)

Verweise

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

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

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100 mg

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GNF-6

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

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GNF-6 Related Classifications

HY-160478 Related Classifications