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AB142082

NVP-TAE684, ALK inhibitor

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(1 Publication)

MW 614.2 Da, Purity >98%. Highly potent, selective ALK inhibitor in vitro (IC50 = 2 nM). Suppresses lymphomagenesis in vivo. Down-regulates CD30 expression. Antitumor agent. Potent LRRK2 kinase inhibitor (IC50 = 7.8 nM).

View Alternative Names

ALK tyrosine kinase receptor, ALK/EML4 fusion gene, included, ALK/NPM1 fusion gene, included, ALK_HUMAN, Alpha-PAK, Anaplastic lymphoma kinase, Anaplastic lymphoma kinase Ki1, B55, Beta PAK, CAM kinase II delta, CAMK 2, CAMK 2B, CAMK 2d, CAMK2G, CAMKA, CD 246, CD246 antigen, CDKN1A, CaM kinase II, CaM kinase II alpha, CaM kinase II beta, CaM kinase II gamma, CaM kinase II subunit alpha, CaMK-II subunit alpha, Calcium / calmodulin dependent protein kinase II delta, Calcium/calmodulin dependent protein kinase II gamma, Calcium/calmodulin-dependent protein kinase II-alpha, Calcium/calmodulin-dependent protein kinase type II subunit alpha, Camk2a, EC 2.7.10.1, EC 2.7.11.1, GCK family kinase MiNK, GSD9C, Gamma-PAK, Germinal center kinase like kinase, Germinal center kinase-related protein kinase, KCC2A_HUMAN, KHS, KI 1, Kinase homologous to SPS1/STE20, MAP4K3, MAPK/ERK kinase kinase kinase 3, MAPK/ERK kinase kinase kinase 5, MAPK/ERK kinase kinase kinase 6, MAPKKKK3, MEK (MAP/ERK) kinase kinase 6, MEK kinase kinase 3, MEK kinase kinase 5, MEK kinase kinase 6, MEKKK 3, MEKKK 5, MEKKK6, MGC21111, MINK, MRX30, MRX47, Misshapen NIKs Related kinase, Misshapen like kinase 1, Misshapen/NIK related kinase, Mitogen activated protein kinase kinase kinase kinase 6, NBLST 3, OPHN3, Oligophrenin 3, P21 (CDKN1A) activated kinase 2, P21 (CDKN1A) activated kinase 3, P21 protein (Cdc42/Rac) activated kinase 1, P21 protein (Cdc42/Rac) activated kinase 3, P21/Cdc42/Rac1 activated kinase 1 (yeast Ste20 related), P58, PAK alpha, PAK3beta, PAK65, PAKgamma, PHK gamma LT, PHK gamma T, PSK C3, Phosphorylase b kinase gamma catalytic chain testis/liver isoform, Phosphorylase b kinase gamma catalytic chain, liver/testis isoform, Phosphorylase kinase catalytic subunit gamma 2, Phosphorylase kinase gamma subunit 2, Phosphorylase kinase subunit gamma 2, Phosphorylase kinase, gamma 2 (testis), Phosphorylase kinase, gamma 2 (testis/liver), RAB8IPL1, RP23-122P1.6, S6/H4 kinase, STE20 homolog, yeast, Serine/threonine protein kinase PAK 2, Serine/threonine protein kinase PAK 3, Serine/threonine protein kinase PHKG2, Serine/threonine-protein kinase PAK 1, TCRZ, TFG/ALK, Ysk2, ZC3, anaplastic lymphoma kinase (Ki-1), anaplastic lymphoma receptor tyrosine kinase, bPAK, calcium/calmodulin-dependent protein kinase II beta, hMINK, hPAK3, mitogen-activated protein kinase kinase kinase kinase 3, mutant anaplastic lymphoma kinase, p21 activated kinase 3, p21 protein (Cdc42/Rac)-activated kinase 2, p21-activated kinase 1, p21-activated kinase 2, p21/Cdc42/Rac1-activated kinase 1 (STE20 homolog, yeast), p65-PAK

1 Images
Chemical Structure - NVP-TAE684, ALK inhibitor (AB142082)
  • Chemical Structure

Lab

Chemical Structure - NVP-TAE684, ALK inhibitor (AB142082)

2D chemical structure image of ab142082, NVP-TAE684, ALK inhibitor

Key facts

CAS number

761439-42-3

Purity

>98%

Form

Solid

form

Molecular weight

614.2 Da

Molecular formula

C<sub>3</sub><sub>0</sub>H<sub>4</sub><sub>0</sub>ClN<sub>7</sub>O<sub>3</sub>S

PubChem

16038120

Nature

Synthetic

Solubility

Soluble in DMSO

Biochemical name

5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)pyrimidine-2,4-diamine

Biological description

Highly potent, selective ALK inhibitor in vitro (IC50 = 2 nM). Suppresses lymphomagenesis in vivo. Down-regulates CD30 expression. Antitumor agent. Potent LRRK2 kinase inhibitor (IC50 = 7.8 nM).

Canonical smiles

CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC

InChi

InChI=1S/C30H40ClN7O3S/c1-21(2)42(39,40)28-8-6-5-7-26(28)33-29-24(31)20-32-30(35-29)34-25-10-9-23(19-27(25)41-4)37-13-11-22(12-14-37)38-17-15-36(3)16-18-38/h5-10,19-22H,11-18H2,1-4H3,(H2,32,33,34,35)

InChiKey

QQWUGDVOUVUTOY-UHFFFAOYSA-N

IUPAC Name

5-chloro-2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine

Product details

This product is manufactured by BioVision, an Abcam company and was previously called 1683 NVP-TAE684. 1683-5 is the same size as the 5 mg size of ab142082.

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate long-term storage conditions
-20°C
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

ALK also known as Anaplastic Lymphoma Kinase is a receptor tyrosine kinase with a molecular mass of approximately 176 kDa. ALK plays an important role in cell signaling and is involved in the regulation of cell growth. It predominantly expresses in the nervous system but also appears in other tissues like the liver and small intestine. The PAK proteins including PAK1 PAK2 and PAK3 function as serine/threonine kinases important for various cellular processes and are expressed in tissues such as the brain and heart. Other targets in this group like MAP4K6 CaMKII PHKG2 MAP4K5 and MAP4K3/GLK function as kinases participating in signal transduction.
Biological function summary

These proteins help regulate critical cellular events like differentiation apoptosis and cytoskeletal reorganization. ALK often forms part of signaling complexes that control cellular communication. CaMKII which is calcium/calmodulin-dependent protein kinase II uniquely regulates synaptic signaling and memory function. PAK proteins mediate pathways that control cytoskeletal dynamics while MAP4K proteins participate in MAP kinase pathways that regulate cell proliferation and survival.

Pathways

These kinases integrate into significant signaling cascades such as the MAPK/ERK pathway and the PI3K/Akt pathway. The MAPK/ERK pathway involving proteins like MAP4K6 and MAP4K5 plays an important role in transmitting signals from growth factors outside the cell to the DNA in the nucleus affecting cell division and differentiation. PAK proteins also link to the PI3K/Akt pathway which influences many cellular processes including metabolism and survival. These pathways emphasize their influence in critical regulatory processes in the cell.

ALK mutations and rearrangements associate strongly with certain cancers such as non-small cell lung cancer and anaplastic large cell lymphoma. The aberrant activation of ALK leads to uncontrolled cell proliferation and survival which is a hallmark of cancer. PAK proteins relate to neurological disorders like Alzheimer's due to their role in cytoskeletal regulation and neuronal signaling. In these diseases interactions with other proteins like EGFR in the case of ALK and tau proteins for PAK1 highlight their relevance in disease mechanisms.

Product protocols

Publications (1)

Recent publications for all applications. Explore the full list and refine your search

The Journal of neuroscience : the official journal of the Society for Neuroscience 40:1232-1247 PubMed31882403

2019

Midkine-a Is Required for Cell Cycle Progression of Müller Glia during Neuronal Regeneration in the Vertebrate Retina.

Applications

Unspecified application

Species

Unspecified reactive species

Mikiko Nagashima,Travis S D'Cruz,Antoinette E Danku,Doneen Hesse,Christopher Sifuentes,Pamela A Raymond,Peter F Hitchcock
View all publications

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