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> ASP3026 [1097917-15-1]

ASP3026 [1097917-15-1]

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Referencia HY-13326-5mg

embalaje : 5mg

Marca : MedChemExpress

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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]
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]
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
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.

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.
Pureza y Documentación
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