| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Purity: ≥98%
GSK 626616 is a novel, potent, and orally bioavailable YAK3/DYRK3 kinase inhibitor with IC50 of 0.7 nM for DYRK3. Possibly used to treat anemia brought on by chemotherapy, it is a chemoprotective agent.
| Targets |
DYRK3 (IC50 = 0.72 nM)
|
|---|---|
| ln Vitro |
GSK-626616 eliminates the phosphorylation of S6K1 at Thr389 in nonstimulated HeLa cells. In HeLa cells stimulated with insulin and EGF, GSK-626616 decreases the phosphorylation of S6K1 at Thr389, indicating a reduction in mTORC1 activity[2].
In serum-deprived HeLa cells, GSK-626616 decreases the phosphorylation of PRAS40 at Thr246 that is induced by EGF. GSK-626616 enhances PRAS40's binding to mTORC1[2]. |
| References |
| Molecular Formula |
C18H10CL2N4OS
|
|---|---|
| Molecular Weight |
401.269199848175
|
| Exact Mass |
399.995
|
| Elemental Analysis |
C, 53.88; H, 2.51; Cl, 17.67; N, 13.96; O, 3.99; S, 7.99
|
| CAS # |
1025821-33-3
|
| Related CAS # |
1025821-33-3
|
| PubChem CID |
135416229
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.6±0.1 g/cm3
|
| Boiling Point |
574.8±60.0 °C at 760 mmHg
|
| Flash Point |
301.4±32.9 °C
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
| Index of Refraction |
1.755
|
| LogP |
4.16
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
26
|
| Complexity |
604
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1C=CC=C(C=1/N=C1/NC(/C(=C/C2C=CC3C(C=2)=NC=CN=3)/S/1)=O)Cl
|
| InChi Key |
RJPNRXFBYZVRIB-DHDCSXOGSA-N
|
| InChi Code |
InChI=1S/C18H10Cl2N4OS/c19-11-2-1-3-12(20)16(11)23-18-24-17(25)15(26-18)9-10-4-5-13-14(8-10)22-7-6-21-13/h1-9H,(H,23,24,25)/b15-9-
|
| Chemical Name |
(5Z)-2-(2,6-dichlorophenyl)imino-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolidin-4-one
|
| Synonyms |
GSK626616; GSK 626616; GSK-626616
|
| HS Tariff Code |
2934.99.9001
|
| 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) |
DMSO: 20~50 mg/mL (49.9~124.6 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (12.46 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4921 mL | 12.4604 mL | 24.9209 mL | |
| 5 mM | 0.4984 mL | 2.4921 mL | 4.9842 mL | |
| 10 mM | 0.2492 mL | 1.2460 mL | 2.4921 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 |
| NCT00443170 | Completed | Drug: GSK626616, placebo , midazolam Drug: omeprazole, caffeine , flurbiprofen, rosiglitazone |
Healthy Subjects Anaemia |
GlaxoSmithKline | November 2006 | Phase 1 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA