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> ASP3026 [1097917-15-1]

ASP3026 [1097917-15-1]

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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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ASP3026 Estructura química

ASP3026 Estructura química

No. CAS : 1097917-15-1

This product is a controlled substance and not for sale in your territory.

Based on 5 publication(s) in Google Scholar

Ver todos los productos específicos de isoformas Caspase:

Ver todas las isoformas
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

Ver todos los productos específicos de isoformas PARP:

Ver todas las isoformas
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

Ver todos los productos específicos de isoformas STAT:

Ver todas las isoformas
STAT3 STAT5 STAT6 STAT1

Ver todos los productos específicos de isoformas Akt:

Ver todas las isoformas
Akt Akt1 Akt2 Akt3

Ver todos los productos específicos de isoformas JNK:

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JNK1 JNK2 JNK3 JNK
Descripciòn

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[1][2][3][4].

IC50 & Target

ROS

 

ACK

 

Caspase-3

 

PARP1

 

IGF-1R

 

STAT3

 

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]
In Vitro

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.

ASP3026 Related Antibodies

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.
In Vivo

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.
Ensayo clínico
Peso molecular

580.74

Fòrmula

C29H40N8O3S
No. CAS

1097917-15-1
Appearance

Solid

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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7219 mL 8.6097 mL 17.2194 mL
5 mM 0.3444 mL 1.7219 mL 3.4439 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Calculadora de molaridad

  • Calculadora de dilución

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación

Purity: 99.88%

SDS (393 KB)

COA (247 KB) LCMS (109 KB)

Instrucciones de manejo (2659 KB)
Referencias

  • [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]

  • [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.

    [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.

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

    [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.

Complete Stock Solution Preparation Table

* 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.

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
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ASP3026 Related Classifications

  • Protein Tyrosine Kinase/RTK Apoptosis Epigenetics Cell Cycle/DNA Damage Stem Cell/Wnt JAK/STAT Signaling PI3K/Akt/mTOR MAPK/ERK Pathway
  • Anaplastic lymphoma kinase (ALK) Apoptosis ROS Kinase Caspase PARP IGF-1R STAT Akt JNK
Help & FAQs

Keywords:

ASP30261097917-15-1ASP 3026ASP-3026Anaplastic lymphoma kinase (ALK)ApoptosisROS KinaseCaspasePARPIGF-1RSTATAktJNKAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246poly ADP ribose polymerase Insulin-like growth factor-1 receptorPKBProtein kinase Bc-Jun N-terminal kinaseapoptosisanticancerNCI-H2228 cellnon-small cell lung cancer (NSCLC)NPM-ALK+ T-cellanaplastic large-cell lymphoma (ALCL)proliferationcell viabilityInhibitorinhibitorinhibit

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