|Description||This active molecular is a selective inhibitor of ALK(anaplastic lymphoma kinase)which is a target found in NSCLC (metastatic non-small cell lung cancer). The IC50 value is 200 pM in ALK enzymatic assays and 25 nM in cells. It less potently inhibits IGF-1R, InsR, and STK22D and IC50 value is 8, 7, and 23 nM. LDK378 is also minimally effective against a panel of other kinases. In Sep 2016, Interim adverse events and efficacy data from phase III ASCEND-4 trial in non small cell lung cancer released by Novartis. In Oct 2016, efficacy data from the phase III ASCEND-3 and ASCEND-5 trial in non small cell lung cancer was presented.|
|B0084-462148||250 mg||$298||In stock|
|Appearance||A crystalline solid|
|Synonyms||5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine， LDK378,Zykadia,1380575-43-8 (2HCl), 1190399-48-4 (xHCl).|
|Solubility||Soluble in DMSO|
|Application||Non small cell lung cancer|
|Quality Standard||In-house standard|
|Shelf Life||2 month in rt, long time|
|Current Developer||Novartis; University of Texas Southwestern Medical Center|
LDN193189 is a selective and potent ALK inhibitor with potential anticancer activity.
AZD-3463 is a potent ALK/IGF1R inhibitor with potential anticancer activity.
CEP-14083 is a ALK inhibitor. It has a potent activity against ALK in enzymatic assays (IC50 = 11 nmol/L). CEP-14083 can also inhibit the insulin receptor at a ...
CEP-14513 is a ALK inhibitor. It shows ALK inhibitory activity in both in vitro enzymatic assay (IC50 = 5 nM) and cell-based assays of ALK tyrosine phosphorylat...
NVP-TAE684 is a highly potent and selective small-molecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC(50) valu...
HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM.
DMH-1 is a second-generation small molecule BMP inhibitor based on dorsomorphin. DMH-1 effectively inhibits the bone morphogenic protein (BMP) ALK2 receptor (IC...
CEP-28122 is a Highly Potent and Selective Orally Active Inhibitor of Anaplastic Lymphoma Kinase with Antitumor Activity in Experimental Models of Human Cancers...
TPX-0005 is an orally available and potent ATP-competitive inhibitor of ALK/ROS1/TRK (IC50= 5.3 nM for SRC, IC50= 1.01 nM, 1.26 nM and 1.08 nM for mutant ALKs i...
AP26113 is an orally available inhibitor of receptor tyrosine kinases anaplastic lymphoma kinase (ALK) and the epidermal growth factor receptor (EGFR) with pote...
Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK. Crizotinib inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM). Crizotinib is use...
Alectinib, also known as AF802, or CH5424802 or RO5424802, is a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, showing ...
ASP3026 is a novel and selective inhibitor for the ALK kinase. ASP3026 potently inhibited ALK kinase activity and was more selective than crizotinib in a Tyr-ki...
LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM. There are currently no effective therapi...
LDN-212854 is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2. LDN-212854 exhibits some selectivity for ALK2 in preference to other...
Belizatinib is inhibitor of both anaplastic lymphoma kinase (ALK) and tropomyosin-related kinases (TRK). Belizatinib can bind to and inhibit both ALK and TRK ki...
IN-1130 is a selective ALK5 inhibitor with >100 fold selectivity over p38α and a panel of 26 other serine/threonine and tyrosine kinases. It also inhibit phosph...
ALK inhibitor 1
ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.
Brigatinib, is an orally active, also known as AP-26113, potent and selective Dual ALK/EGFR inhibitor. AP26113 binds to and inhibits ALK kinase(ALK belongs to t...
LDN193189 HCl is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I ...