ASP3026

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].

Product Specifications

CAS Number

[1097917-15-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Akt; Anaplastic lymphoma kinase (ALK) ; Apoptosis; Caspase; IGF-1R; JNK; PARP; ROS Kinase; STAT

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ASP3026.html

Purity

99.88

Solubility

DMSO : 20 mg/mL (ultrasonic)

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

Molecular Formula

C29H40N8O3S

Molecular Weight

580.74

Precautions

H302, H315, H319, H335

References & Citations

[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.