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Art. -Nr.: HY-128602

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c-Kit-IN-2

c-Kit-IN-2 is a c-KIT inhibitor with an IC₅₀ of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI₅₀s of 3, 1, and 2 nM, respectively.

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CAS. Nr.: 2121515-37-3
Formel: C₂₅H₂₉N₉O₂S
Molecular Weight:519.62

Speicherung:

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

Data Sheet (266 KB)

c-Kit-IN-2 Chemical Structure

CAS. Nr.: 2121515-37-3

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 82 nM (c-KIT)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	14.6 μM Compound: 10a	Antiproliferative activity against human A549 assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human A549 assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 30968693]
Detroit 551	GI₅₀	>10 μM Compound: 10a	Antiproliferative activity against human Detroit 551 assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human Detroit 551 assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 30968693]
GIST430	GI₅₀	1 nM Compound: 10a	Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by methylene blue staining based ass Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by methylene blue staining based ass	[PMID: 30968693]
GIST430	GI₅₀	1 nM Compound: 10a	Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by MTS assay Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by MTS assay	[PMID: 30968693]
GIST48	GI₅₀	2 nM Compound: 10a	Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by methylene blue staining based assay Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by methylene blue staining based assay	[PMID: 30968693]
GIST48	GI₅₀	2 nM Compound: 10a	Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by MTS assay Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by MTS assay	[PMID: 30968693]
GIST882	GI₅₀	3 nM Compound: 10a	Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by methylene blue staining based assay Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by methylene blue staining based assay	[PMID: 30968693]
GIST882	GI₅₀	3 nM Compound: 10a	Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by MTS assay Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by MTS assay	[PMID: 30968693]
GISTT1	GI₅₀	2.2 nM Compound: 10a	Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 del mutation assessed as reduction in cell viability by methylene blue staining based assay Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 del mutation assessed as reduction in cell viability by methylene blue staining based assay	[PMID: 30968693]
GISTT1	GI₅₀	2.2 nM Compound: 10a	Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 deletion mutant assessed as reduction in cell viability by MTS assay Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 deletion mutant assessed as reduction in cell viability by MTS assay	[PMID: 30968693]
PC-3	GI₅₀	>20 μM Compound: 10a	Antiproliferative activity against human PC3 assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human PC3 assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 30968693]
Sf9	IC₅₀	69 nM Compound: 10a	Inhibition of unactivated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 30 Inhibition of unactivated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 30	[PMID: 30968693]
Sf9	IC₅₀	82 nM Compound: 10a	Inhibition of recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation measured after 150 mins in pr Inhibition of recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation measured after 150 mins in pr	[PMID: 30968693]
Sf9	IC₅₀	92 nM Compound: 10a	Inhibition of ATP-activated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 3 Inhibition of ATP-activated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 3	[PMID: 30968693]

Chemical Information

CAS. Nr. 2121515-37-3
Molecular Weight 519.62
Formel C₂₅H₂₉N₉O₂S
SMILES

CCN1CCN(C2=CC(NC3=NC=C(C4=CC=C(NC(NC5=NOC(CC)=C5)=O)C=C4)S3)=NC=N2)CC1
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 (266 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]. Wu TS, et al. Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. J Med Chem. 2019 Apr 25;62(8):3940-3957. [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.

Keywords

100 mg

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