GSK2126458
| Code | Size | Price |
|---|
| SYN-1126-M100 | 100 mg | Enquire |
Quantity:
| SYN-1126-M001 | 1 mg | £180.00 |
Quantity:
| SYN-1126-M005 | 5 mg | £268.00 |
Quantity:
| SYN-1126-M010 | 10 mg | £420.00 |
Quantity:
| SYN-1126-M050 | 50 mg | £1,240.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Documents
Further Information
Alternate Names/Synonyms:
HYR-582
Appearance:
Solid.
CAS:
1086062-66-9
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS07
Hazards:
H303, H317, H333
InChi:
InChI=1S/C25H17F2N5O3S/c1-35-25-23(32-36(33,34)24-5-3-18(26)12-21(24)27)11-17(13-29-25)15-2-4-22-20(10-15)19(7-8-28-22)16-6-9-30-31-14-16/h2-14,32H,1H3
InChiKey:
CGBJSGAELGCMKE-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 1086062-66-9. Formula: C25H17F2N5O3S. MW: 505.5. GSK2126458 is an orally available selective inhibitor of the class I phosphoinositide 3-kinase (PI3K) enzymesand MTOR1/2 complexes. GSK2126458 can inhibit PI3K-alpha (p85alpha/p110alpha) with IC(50) of 0.04nM. GSK2126458 has Ki values in the picomolar range for each of the class I PI3K isoforms and MTOR1/2 complexes. GSK2126458 has potent in vitro and in vivo growth-inhibitory effects on cancer cells. In comparison with other clinical PI3K inhibitors, GSK2126458 is around 100-fold more potent than BEZ235 (6nM). GSK2126458 also a low picomolar inhibitor of the common activating mutants of p110R ( E542K, E545K, and H1047R ) with Ki of 0.008nM, 0.008nM and 0.009nM in human cancer. In mechanistic cellular assays, GSK2126458 caused a significant reduction in the levels of pAKT-S473 with remarkable potency. Consistent with its activity against both PI3K R and mTOR, GSK2126458 also inhibits phosphorylation of AKT-T308 and p70S6K at low nanomolar concentrations. GSK2126458 induces a G1 cell cycle arrest and inhibits cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines.
Molecular Formula:
C25H17F2N5O3S
Molecular Weight:
505.5
Package Type:
Plastic Vial
Precautions:
P261, P272, P280, P302, P352, P333, P313, P321, P363, P501
Product Description:
GSK2126458 is an orally available selective inhibitor of the class I phosphoinositide 3-kinase (PI3K) enzymesand MTOR1/2 complexes. GSK2126458 can inhibit PI3K-alpha (p85alpha/p110alpha) with IC(50) of 0.04nM. GSK2126458 has Ki values in the picomolar range for each of the class I PI3K isoforms and MTOR1/2 complexes. GSK2126458 has potent in vitro and in vivo growth-inhibitory effects on cancer cells. In comparison with other clinical PI3K inhibitors, GSK2126458 is around 100-fold more potent than BEZ235 (6nM). GSK2126458 also a low picomolar inhibitor of the common activating mutants of p110R ( E542K, E545K, and H1047R ) with Ki of 0.008nM, 0.008nM and 0.009nM in human cancer. In mechanistic cellular assays, GSK2126458 caused a significant reduction in the levels of pAKT-S473 with remarkable potency. Consistent with its activity against both PI3K R and mTOR, GSK2126458 also inhibits phosphorylation of AKT-T308 and p70S6K at low nanomolar concentrations. GSK2126458 induces a G1 cell cycle arrest and inhibits cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines.
Purity:
>95%
Signal word:
Warning
Solubility Chemicals:
Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
References
The PDBbind database: collection of binding affinities for protein-ligand complexes with known three-dimensional structures. R. Wang, et al.; J. Med. Chem. 47, 2977 (2004) | Comparison of the effects of the PI3K/mTOR inhibitors NVP-BEZ235 and GSK2126458 on tamoxifen-resistant breast cancer cells: E. Leung, et al.; Cancer Biol. Ther. 11, 938 (2011)
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