country

Change Language

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

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

製品番号: HY-128602

Copy Link Print Information

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 2121515-37-3
分子式: C₂₅H₂₉N₉O₂S
分子量:519.62

保管条件:

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

Data Sheet (266 KB)

c-Kit-IN-2 構造式

CAS 番号: 2121515-37-3

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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]

化学情報

CAS 番号 2121515-37-3
分子量 519.62
分子式 C₂₅H₂₉N₉O₂S
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (266 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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

お問い合わせ在庫あり