country

Change Language

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

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

製品番号: HY-151155

Copy Link Print Information

ALK-IN-23

ALK-IN-23 is a potent ALK inhibitor with IC₅₀ values of 1.6 nM, 0.71 nM and 1.3 nM for ALK^WT, ALK^L1196M and ALK^G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity.

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: 3033549-18-4
分子式: C₂₆H₂₉ClN₈O₃S
分子量:569.08

保管条件:

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

Data Sheet (274 KB)

ALK-IN-23 構造式

CAS 番号: 3033549-18-4

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
- 体外実験
- 体内実験
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: 1.6 nM (ALK^WT), 0.71 nM (ALK^L1196M), 1.3 nM (ALK^G1202R)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1.33 μM Compound: Y28	Antiproliferative activity against EGFR-positive human A549 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against EGFR-positive human A549 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
HCT-116	IC₅₀	1.56 μM Compound: Y28	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
KARPAS-299	IC₅₀	0.015 μM Compound: Y28	Antiproliferative activity against NPM-ALK-positive human KARPAS-299 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against NPM-ALK-positive human KARPAS-299 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
MCF7	IC₅₀	2.22 μM Compound: Y28	Antiproliferative activity against human MCF7 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
NCI-H1581	IC₅₀	1.87 μM Compound: Y28	Antiproliferative activity against human NCI-H1581 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human NCI-H1581 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
NCI-H2228	IC₅₀	0.017 μM Compound: Y28	Antiproliferative activity against EML4-ALK-positive human NCI-H2228 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against EML4-ALK-positive human NCI-H2228 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
NCI-H3122	IC₅₀	0.012 μM Compound: Y28	Antiproliferative activity against EML4-ALK-positive human NCI-H3122 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against EML4-ALK-positive human NCI-H3122 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
NCI-H460	IC₅₀	8.21 μM Compound: Y28	Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
PC-3	IC₅₀	1.23 μM Compound: Y28	Antiproliferative activity against human PC-3 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human PC-3 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]

体外実験

ALK-IN-23 (compound Y28) (0-5 μM; 72h) has highly inhibitory activity against H3122, H2228, Karpas299 and A549^[1].
ALK-IN-23 (25-100 nM; 3 days) clearly reduces the number of H2228 cell colonies, and almost completely abolishes the formation of colonies at 100 nM^[1].
ALK-IN-23 (100-200 nM; 48 h) facilitates the apoptosis of H2228 cells^[1].
ALK-IN-23 (5-10 nM; 24 and 48 h) is effective to block the migration of most cells at a dose of 10 nM^[1].
ALK-IN-23 (25-100 nM; overnight) significantly increases the percentage of cells in the G2 phase^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

H3122, H2228, Karpas299 and A549
Concentration:

0-5 μM
Incubation Time:

72 h
Result:

Exhibited highly inhibitory activity against H3122, H2228, Karpas299 and A549 with IC₅₀s of 12 nM, 17 nM, 15 nM and 1.33 μM.

Apoptosis Analysis^[1]

Cell Line:

H2228 cells
Concentration:

100 nM, 200 nM
Incubation Time:

48 h
Result:

Facilitated the apoptosis of H2228 cells in a dose dependent manner and exhibited a more pro-apoptotic effect than that of Ceritinib (HY-15656).

Cell Migration Assay ^[1]

Cell Line:

H2228 cells
Concentration:

5 nM and 10 nM
Incubation Time:

24 and 48 h
Result:

Blocked the migration of most cells at a dose of 10 nM (migration rate: 24 h 2.31%, 48 h: 5.01%).

Cell Cycle Analysis^[1]

Cell Line:

H2228 cells
Concentration:

25 nM, 50 nM, 100 nM
Incubation Time:

Overnight
Result:

Significantly increased the percentage of cells in the G2 phase from 11.28% to 73.23% in a dramatic dose-dependent manner, accompanied by a resultant loss of G1-and S-phase populations.

体内実験

ALK-IN-23 notes a moderate half-life of 16.3 min and a high intrinsic liver clearance of 152.9 mL/min/kg in rats^[1].
ALK-IN-23 (25 and 50 mg/kg; IG; once every 2 days; for 14 days) exhibited gentle antitumor efficacy and no significant weight loss in H2228 xenograft mice model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female BALB/c nude mice (5×10⁶ cells H2228 cells suspended in serum-free media were injected into the flanks)^[1]
Dosage:

25 and 50 mg/kg
Administration:

IG; once every 2 days; for 14 days
Result:

Presented moderate antitumor efficacy with the tumor growth inhibition (TGI) of 70.46% at 50 mg/kg.
Possessed gentle antitumor efficacy and exhibited no significant weight loss.

化学情報

CAS 番号 3033549-18-4
分子量 569.08
分子式 C₂₆H₂₉ClN₈O₃S
SMILES

CC(S(=O)(C1=CC=CC=C1NC2=NC(NC3=CC=C4C(NN=C4NC(CN5CCCC5)=O)=C3)=NC=C2Cl)=O)C
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 (274 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]. Yang J, et al. Design, synthesis and antitumor evaluation of ATP dual-mimic 2,4-diarylaminopyrimidine and aminoindazole conjugates as potent anaplastic lymphoma kinase inhibitors. Eur J Med Chem. 2022 Jul 31;241:114626. [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

MOQ

Minimum order quantity

100 mg

お問い合わせ在庫あり

Other size

お問い合わせ