ASP3026 free base · Synonyms: ASP-3026 · ASP 3026

ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase.

For research use only. Not for human or veterinary use.

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

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

ASP3026 structure

CAS No.: 1097917-15-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 320.00	BP-02463-250mg	In stock	Get quote
500 mg	USD 510.00	BP-02463-500mg	In stock	Get quote
1 g	USD 810.00	BP-02463-1g	In stock	Get quote
2 g	USD 1,310.00	BP-02463-2g	In stock	Get quote
3 g	USD 1,570.00	BP-02463-3g	In stock	Get quote
5 g	USD 2,090.00	BP-02463-5g	In stock	Get quote
10 g	USD 3,350.00	BP-02463-10g	In stock	Get quote

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Description

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 .

Biological activity

In Vitro ASP3026 decreases the viability, proliferation, and colony formation, as well as induced apoptotic cell death of NPM-ALK+ ALCL cells. 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. 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. 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). 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.

Identifiers

SMILES: COC1=CC(=CC=C1NC1=NC(NC2=CC=CC=C2S(=O)(=O)C(C)C)=NC=N1)N1CCC(CC1)N1CCN(C)CC1
InChIKey: MGGBYMDAPCCKCT-UHFFFAOYSA-N

Specifications

MW (average): 580.7450
Formula: C₂₉H₄₀N₈O₃S
CAS No.: 1097917-15-1
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 year;

Solubility

Soluble in DMSO

Documents

References

[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.

Same target

Search Anaplastic lymphoma kinase (ALK)

Same research area

Search Cancer