製品番号: HY-13326

ASP3026

6 Cited Publications

カスタマーレビュー

Based on 6 publication(s) in Google Scholar

ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC₅₀ value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, AKT and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. ASP3026 can be used in anti-tumor research.

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純度: 99.88%
CAS 番号: 1097917-15-1
分子式: C₂₉H₄₀N₈O₃S
分子量:580.74

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ASP3026 構造式

CAS 番号: 1097917-15-1

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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
- 臨床実験
化学情報
Publications (6)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

ROS

ACK

Caspase-3

PARP1

IGF-1R

STAT3

Caspase アイソフォーム固有の製品をすべて表示 :

PARP アイソフォーム固有の製品をすべて表示 :

STAT アイソフォーム固有の製品をすべて表示 :

Akt アイソフォーム固有の製品をすべて表示 :

JNK アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	1508 nM Compound: 20; ASP3026	Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 33243531]
BaF3	IC₅₀	17 nM Compound: 2; ASP3026	Inhibition of EML4-fused ALK variant 1 (unknown origin) expressed in mouse BAF3 cells using peptide substrate measured after 1 hr by HTRF assay Inhibition of EML4-fused ALK variant 1 (unknown origin) expressed in mouse BAF3 cells using peptide substrate measured after 1 hr by HTRF assay	[PMID: 30878193]
BaF3	IC₅₀	323.9 nM Compound: 20; ASP3026	Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 33243531]
NCI-H2228	IC₅₀	64.8 nM Compound: Chemical probe: ASP3026	Antiproliferative activity against human NCI-H2228 cell spheroids assessed as reduction in cell growth measured after 5 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human NCI-H2228 cell spheroids assessed as reduction in cell growth measured after 5 days by celltiter-glo luminescent cell viability assay	[PMID: 24419060]

体外実験

ASP3026 decreases the viability, proliferation, and colony formation, as well as induced apoptotic cell death of NPM-ALK+ ALCL cells^[2].
ASP3026 significantly reduces the proliferation of 293T cells transfected with NPM-ALK mutants that are resistant to Crizotinib (HY-50878) and downregulates tyrosine phosphorylation of these mutants^[2].
ASP3026 (1-4 µg/ml, 48 h) is a novel inhibitor of red blood cell membrane scrambling following energy depletion and oxidative stress, thereby counterbalancing suicidal red blood cell death and subsequent development of anemia^[3].
ASP3026 (100 nM, 1000 nM, 5 days) inhibits ALK activity in a competitive manner with ATP, and its inhibition profile is different from that of the dual ALK/MET inhibitor Crizotinib (HY-50878)^[4].

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

Western Blot Analysis^[2]

Cell Line:

NPM-ALK⁺ ALCL cell, 50-80 μg total proteins
Concentration:

0.1-2.5 μM
Incubation Time:

24-72 h
Result:

Significantly decreased the activity of NPM-ALK tyrosine kinase and the tyrosine phosphorylation levels at Y646 and Y664, and decreased the phosphorylation levels of IGF-IR, STAT3, AKT and JNK proteins, the target proteins of NPM-ALK signal transduction.
Successfully induced the cleavage of caspase 3 and PARP, which further indicated that it induced the apoptosis of NPM-ALK⁺ ALCL cells.

Cell Viability Assay^[2]

Cell Line:

NPM-ALK+ T-cell ALCL cell lines Karpas 299, SU-DHL-1, SUP-M2, SR-786, DEL
Concentration:

0.1-2.5 μM
Incubation Time:

24-72 h
Result:

At 48 h, the IC₅₀ values of SU-DHL-1, SUP-M2, SR-786, Karpas 299 and DEL were 0.4 µM, 0.75 µM, 1.0 µM, 2.5 µM and greater than 3.0 µM, respectively.
Significantly reduced the viability of lymphoma cells than that of T lymphocytes.
At 72 h, the IC₅₀ values of SU-DHL-1, SUP-M2, SR-786, Karpas 299 and DEL were 0.3 µM, 0.75 µM, 0.75 µM, 2.5 µM and 0.5 µM, respectively.

Cell Proliferation Assay^[4]

Cell Line:

NCI-H2228 NSCLC
Concentration:

100 nM, 1000 nM
Incubation Time:

5 days
Result:

Inhibited the growth of ALK-dependent cells.
Inhibited the growth of NCI-H2228 cells with an IC₅₀ value of 64.8 nM.

体内実験

ASP3026 (30 mg/kg daily for 10 weeks, p.o.) inhibits the growth of NPM-ALK⁺ ALCL tumor cells in mice^[2].
ASP3026 (10 mg/kg daily for 5 days, p.o.) can enhance the antitumor activity of Paclitaxel (HY-B0015) and Pemetrexed (HY-10820). When used alone, it can induce tumor regression and prolong survival in non-small cell lung cancer model mice, and does not affect the body weight of non-small cell lung cancer model mice^[4].

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

Animal Model:

Female C.B-17 SCID mice of systemic xenograft lymphoma model^[2]
Dosage:

30 mg/kg daily for 10 weeks
Administration:

p.o.
Result:

Mice in the ASP3026-interrupted group developed recurrent lymphoma, were subsequently treated with ASP3026 and survived until the end of the study.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1097917-15-1
性状 Solid
分子量 580.74
分子式 C₂₉H₄₀N₈O₃S
Color White to off-white
SMILES

COC(C=C(N1CCC(N2CCN(C)CC2)CC1)C=C3)=C3NC4=NC=NC(NC5=C(S(C(C)C)(=O)=O)C=CC=C5)=N4
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

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Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Pharmaceuticals (Basel)

Therapeutic Implications of Ceritinib in Cholangiocarcinoma beyond ALK Expression and Mutation. [Abstract]

2024 Feb 2;17(2):197. PMID: 38399413
Cell Physiol Biochem

Inhibition of Erythrocyte Cell Membrane Scrambling by ASP3026. [Abstract]

2017;43(2):507-517. PMID: 28930717
SSRN

2025 Sep 19.
Technical University of Munich

24.01.2018.

溶剤 & 溶解度

体外:

DMSO : 20 mg/mL (34.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7219 mL

8.6097 mL

17.2194 mL

5 mM

0.3444 mL

1.7219 mL

3.4439 mL

10 mM

0.1722 mL

0.8610 mL

1.7219 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

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

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濃度濃度

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分子量分子量

希釈計算機

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濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2 mg/mL (3.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2 mg/mL (3.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2 mg/mL (3.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

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 (280 KB)
SDS (393 KB)
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- Deutsch - DE (393 KB)
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- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Discovery of Iikubo K, et, al. N-{2-Methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}-N'-[2-(propane-2-sulfonyl)phenyl]-1,3,5-triazine-2,4-diamine (ASP3026), a Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor. Chem Pharm Bull (Tokyo). 2018;66(3):251-262. [Content Brief]

[2]. George SK, et, al. The ALK inhibitor ASP3026 eradicates NPM-ALK⁺ T-cell anaplastic large-cell lymphoma in vitro and in a systemic xenograft lymphoma model. Oncotarget. 2014 Jul 30;5(14):5750-63. [Content Brief]

[3]. Bhuyan AAM, et, al. Inhibition of Erythrocyte Cell Membrane Scrambling by ASP3026. Cell Physiol Biochem. 2017;43(2):507-517. [Content Brief]

[4]. Mori M, et al. The selective anaplastic lymphoma receptor tyrosine kinase inhibitor ASP3026 induces tumor regression and prolongs survival in non-small cell lung cancer model mice. Mol Cancer Ther. 2014 Feb;13(2):329-40. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7219 mL	8.6097 mL	17.2194 mL	43.0485 mL
	5 mM	0.3444 mL	1.7219 mL	3.4439 mL	8.6097 mL
	10 mM	0.1722 mL	0.8610 mL	1.7219 mL	4.3049 mL
	15 mM	0.1148 mL	0.5740 mL	1.1480 mL	2.8699 mL
	20 mM	0.0861 mL	0.4305 mL	0.8610 mL	2.1524 mL
	25 mM	0.0689 mL	0.3444 mL	0.6888 mL	1.7219 mL
	30 mM	0.0574 mL	0.2870 mL	0.5740 mL	1.4350 mL

ASP3026

6 Cited Publications

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ASP3026

Apoptosis Compound Library

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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

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MedChemExpress（MCE）の使用を引用している文献 ASP3026

Caspase アイソフォーム固有の製品をすべて表示

PARP アイソフォーム固有の製品をすべて表示

STAT アイソフォーム固有の製品をすべて表示

Akt アイソフォーム固有の製品をすべて表示

JNK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (6)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

ASP3026 関連分類

HY-13326 関連分類