| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
GSK126 (GSK-2816126; GSK-2816126A) is a selective and SAM (S-adenosyl-methionine)-competitive inhibitor of EZH2 (Enhancer of zeste homolog 2) methyltransferase with anticancer activity. It inhibits EZH2 with an IC50 of 9.9 nM, and shows >1000-fold selective for EZH2 over other human methyltransferases. It exhibits high antiproliferative activity and in vivo antitumor efficacy.
| ln Vitro |
Regardless of the substrate employed, GSK126 selectively inhibits the activity of both wild-type and mutant EZH2 methyltransferase with a similar degree of efficacy (Ki=0.5-3 nM). It is competitive with S-adenosylmethionine (SAM) but not with peptide substrates. GSK126 has remarkable selectivity towards many other protein classes and other methyltransferases (EZH1, IC50=680 nM) [1]. Three SCLC cell lines were treated with GSK126 to cause growth inhibition. Lu130, H209, and DMS53 SCLC cell lines were treated with 0.5, 2, and 8 μM GSK126, and the WST-8 test was used to examine the growth curves. GSK126 treatment at 8 μM decreased cell proliferation in all three cell lines, but Lu130 and H209 were more susceptible to GSK126, even at lower dosages [2].
|
||
|---|---|---|---|
| ln Vivo |
In female beige SCID mice, GSK126 is given intraperitoneally at a dosage amount of 0.2 mL per 20 g body weight. GSK126 significantly and efficiently suppresses the growth of EZH2 mutant DLBCL xenografts in mice as well as the proliferation of EZH2 mutant DLBCL cell lines[1].
|
||
| Animal Protocol |
|
||
| References |
[1]. McCabe MT, et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature. 2012 Dec 6;492(7427):108-12.
[2]. Sato T, et al. PRC2 overexpression and PRC2-target gene repression relating to poorer prognosis in small cell lung cancer. Sci Rep. 2013 May 29;3:1911 |
| Molecular Formula |
C31H38N6O2
|
|
|---|---|---|
| Molecular Weight |
526.67
|
|
| CAS # |
1346574-57-9
|
|
| Related CAS # |
|
|
| SMILES |
O=C(C1=CC(C2=CC=C(N3CCNCC3)N=C2)=CC4=C1C(C)=CN4[C@@H](C)CC)NCC5=C(C)C=C(C)NC5=O
|
|
| InChi Key |
FKSFKBQGSFSOSM-QFIPXVFZSA-N
|
|
| InChi Code |
InChI=1S/C31H38N6O2/c1-6-22(5)37-18-20(3)29-25(30(38)34-17-26-19(2)13-21(4)35-31(26)39)14-24(15-27(29)37)23-7-8-28(33-16-23)36-11-9-32-10-12-36/h7-8,13-16,18,22,32H,6,9-12,17H2,1-5H3,(H,34,38)(H,35,39)/t22-/m0/s1
|
|
| Chemical Name |
(S)-1-(sec-butyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide
|
|
| Synonyms |
GSK-2816126; GSK 2816126; GSK2816126; GSK126; GSK-126; GSK 126
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8987 mL | 9.4936 mL | 18.9872 mL | |
| 5 mM | 0.3797 mL | 1.8987 mL | 3.7974 mL | |
| 10 mM | 0.1899 mL | 0.9494 mL | 1.8987 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02082977 | Terminated Has Results | Drug: GSK2816126 | Cancer Neoplasms |
GlaxoSmithKline | April 24, 2014 | Phase 1 |
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
