c-Kit-IN-2

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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.

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

c-Kit-IN-2 Chemical Structure

CAS No. : 2121515-37-3

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Description

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 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]
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]
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]
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]
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]
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]
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]
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]
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]

Molecular Weight

519.62

Formula

C₂₅H₂₉N₉O₂S

CAS No.

2121515-37-3

SMILES

CCN1CCN(C2=CC(NC3=NC=C(C4=CC=C(NC(NC5=NOC(CC)=C5)=O)C=C4)S3)=NC=N2)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

c-Kit-IN-2 Related Classifications

Molarity Calculator
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The molarity calculator equation

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

c-Kit-IN-22121515-37-3c-KitSCFRCD117Inhibitorinhibitorinhibit

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c-Kit-IN-2

c-Kit-IN-2 Related Antibodies

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c-Kit-IN-2 Related Classifications

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