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Cat. No.: 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.

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

CAS No.: 2121515-37-3
Formula: C₂₅H₂₉N₉O₂S
Molecular Weight:519.62

Storage:

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

Data Sheet (266 KB)

c-Kit-IN-2 Chemical Structure

CAS No.: 2121515-37-3

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Protocols (2)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

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 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 No. 2121515-37-3
Molecular Weight 519.62
Formula C₂₅H₂₉N₉O₂S
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.

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.

Purity & Documentation

Select Batch:

Purity: 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)

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]

Calculators

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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

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100 mg

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