| Identification | Back Directory | [Name]
N2-[2-Methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-1,3,5-triazine-2,4-diamine | [CAS]
1097917-15-1 | [Synonyms]
CS-286
ASP 3026
ASP 3026; ASP-3026
ASP3026;ASP 3026;ASP-3026
N2-[2-Methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfon
N2-(2-(isopropylsulfonyl)phenyl)-N4-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)-1,3,5-triazine-2,4-diamine
N2-[2-Methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-1,3,5-triazine-2,4-diamine
1,3,5-Triazine-2,4-diamine, N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-
N2-[2-Methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-1,3,5-triazine-2,4-diamine USP/EP/BP
N2-[2-Methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-1,3,5-triazine-2,4-diamine ASP 3026 | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C29H40N8O3S | [MDL Number]
MFCD21609265 | [MOL File]
1097917-15-1.mol | [Molecular Weight]
580.745 |
| Chemical Properties | Back Directory | [Boiling point ]
794.3±70.0 °C(Predicted) | [density ]
1.276 | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥14.53 mg/mL in DMSO; ≥4.9 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
solid | [pka]
8.14±0.42(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
ASP3026 is an ATP-competitive, second-generation ALK inhibitor (IC50 = 3.5 nM) that also inhibits ROS (IC50 = 8.9 nM) and ACK (IC50 = 5.8 nM). It inhibits neuroblastoma-activating ALK mutants F1174L (IC50 = 10 nM) and R1275Q (IC50 = 5.4 nM) and demonstrates antitumor activity in xenograft mouse models. ASP3026 has been shown to overcome crizotinib resistance in non-small cell lung cancer, and is currently being evaluated in clinical trials of patients with ALK-positive solid tumors. | [Uses]
ASP3026 is a novel and selective anaplastic lymphoma kinase (ALK) inhibitor that shows potent anti-tumor activities. ASP3026 also shows potential efficacy for non-small cell lung cancer (NSCLC) and is expected to improve the therapeutic outcomes of patients with cancer with ALK abnormality. Potent ALK inhibitor. | [Definition]
ChEBI: ASP-3026 is a member of the class of diamino-1,3,5-triazines that is 1,3,5-triazine-2,4-diamine in which the amino groups at positions 2 and 4 are respectively carrying 2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl and 2-(propan-2-ylsulfonyl)phenyl substituents. It is a potent inhibitor of anaplastic lymphoma kinase (ALK), Ack and ROS1 activity (IC50 values are 3.5, 5.8 and 8.9 nM respectively) and exhibits anti-cancer properties. It has a role as an antineoplastic agent, an apoptosis inducer, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, an antimalarial and an EC 6.1.1.6 (lysine--tRNA ligase) inhibitor. It is a secondary amino compound, a monomethoxybenzene, a N-methylpiperazine, an aromatic amine, a diamino-1,3,5-triazine, a member of piperidines and a sulfone. | [Enzyme inhibitor]
This potent signal transduction inhibitor (FW = 580.74 g/mol; CAS
1097917-15-1; Solubility: 14 mg/mL DMSO; <1 mg/mL H2O), also known
as N2-[2-methoxy-4-[4- (4-methyl-1-piperazinyl) -1-piperidinyl]phenyl]-N4-
[2-[ (1-methylethyl) sulfonyl]phenyl]-1,3,5-triazine-2,4-diamine, targets
ALK, the Activin receptor-Like Kinase activity of Transforming Growth
Factor-b (TGF-b) receptors, with IC50 of 3.5 nM. ASP3026 inhibits ALK in
an ATP-competitive manner with an inhibitory spectrum that differs from
crizotinib, a dual ALK/MET inhibitor. In patients with non-small cell lung
cancer, a therapeutic target is the EML4-ALK fusion protein, which is
formed between echinoderm microtubule-associated protein like 4 and
ALK as a consequence of the rearrangement of ALK and EML4 genes. In
mice xenografted with EML4-ALK-expressing NCI-H2228 cells, orally
administered ASP3026 is well absorbed in tumor tissues, reaching
concentrations >10-fold higher than those in plasma, and induces tumor
regression with a wide therapeutic margin between efficacious and toxic
doses. In the same mouse model, ASP3026 enhances the antitumor
activities of paclitaxel and pemetrexed without affecting body weight.
ASP3026 also showed potent antitumor activities, including tumor
shrinkage to a undetectable level, in hEML4-ALK transgenic mice and
prolonged survival in mice with intrapleural NCI-H2228 xenografts.
Finally, ASP3026 exhibiL1t1e9d6M potent antitumor activity against cells
expressing EML4-ALK, a mutation conferring resistance to
crizotinib. | [storage]
Store at -20°C | [References]
[1] kuromitsu s, mori m, shimada i, et al. anti-tumor activity of asp3026, a novel and selective alk inhibitor of anaplastic lymphoma kinase (alk).annual meeting of the american association for cancer research (aacr), orlando, fl. 2011.
[2] mori m, ueno y, konagai s, 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. molecular cancer therapeutics, 2014, 13(2): 329-340.
[3] george s k, vishwamitra d, manshouri r, 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, 5(14): 5750-5763. |
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