GSK2126458 (GSK458) - ≥98%, high purity , CAS No.1086062-66-9, Inhibitor of mechanistic target of rapamycin kinase;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit alpha;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit beta;Inhibitor of phosphatidylinositol-4;

Item Number

G127233

Grouped product items
SKU	Size	Availability	Price
G127233-2mg	2mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$34.90
G127233-5mg	5mg	3	$70.90
G127233-10mg	10mg	3	$118.90
G127233-25mg	25mg	2	$267.90
G127233-50mg	50mg	2	$360.90
G127233-100mg	100mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$649.90

Highly potent PI 3-kinase inhibitor; also potent inhibitor of mTOR and DNA-PK

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Basic Description

Synonyms	A25172 \| CHEBI:95093 \| HMS3656D09 \| N-[2-Methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]benzenesulfonamide \| D10718 \| DTXSID10148604 \| 2,4-difluoro-N-(2-(methyloxy)-5-(4-(4-pyridazinyl)-6-quinolinyl)-3-pyridinyl)benzenesulfonamide \| GSK2126458 \| G
Specifications & Purity	Moligand™, ≥98%
Biochemical and Physiological Mechanisms	GSK2126458 (GSK458) is an orally active, highly potent and selective ATP site inhibitor against phosphoinositide 3-kinase (PI3K p110α CI50 = 40 pM; p100 α/δ/γ/β Ki = 19/24/60/130 pM; p110α E542K/E545K/H1047R Ki = 8/8/9 pM), mTOR (mTORC1/C2 Ki = 180/300 pM
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of mechanistic target of rapamycin kinase;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit alpha;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit beta;Inhibitor of phosphatidylinositol-4;
Product Description	GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively.

Names and Identifiers

Pubchem Sid	504770000
Pubchem Sid Url	https://pubchem.ncbi.nlm.nih.gov/substance/504770000
IUPAC Name	2,4-difluoro-N-[2-methoxy-5-(4-pyridazin-4-ylquinolin-6-yl)pyridin-3-yl]benzenesulfonamide
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
InChi Key	CGBJSGAELGCMKE-UHFFFAOYSA-N
Canonical SMILES	COC1=C(C=C(C=N1)C2=CC3=C(C=CN=C3C=C2)C4=CN=NC=C4)NS(=O)(=O)C5=C(C=C(C=C5)F)F
Isomeric SMILES	COC1=C(C=C(C=N1)C2=CC3=C(C=CN=C3C=C2)C4=CN=NC=C4)NS(=O)(=O)C5=C(C=C(C=C5)F)F
Alternate CAS	1086062-66-9
PubChem CID	25167777
MeSH Entry Terms	2,4-difluoro-N-(2-(methyloxy)-5-(4-(4-pyridazinyl)-6-quinolinyl)-3-pyridinyl)benzenesulfonamide;GSK 212;GSK 2126458;GSK-212;GSK-2126458;GSK212;GSK2126458;omipalisib
Molecular Weight	505.5

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

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5 results found

Lot Number	Certificate Type	Date	Item
A2205264	Certificate of Analysis	Oct 10, 2023	G127233
A2205271	Certificate of Analysis	Oct 10, 2023	G127233
A2205276	Certificate of Analysis	Oct 10, 2023	G127233
A2205285	Certificate of Analysis	Oct 10, 2023	G127233
A2205300	Certificate of Analysis	Oct 10, 2023	G127233

Safety and Hazards(GHS)

Pictogram(s)	GHS06, GHS08
Signal	Danger
Hazard Statements	H301:Toxic if swallowed H341:Suspected of causing genetic defects H372:Causes damage to organs through prolonged or repeated exposure H361:Suspected of damaging fertility or the unborn child
Precautionary Statements	P280:Wear protective gloves/protective clothing/eye protection/face protection. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P281:Use personal protective equipment as required. P270:Do not eat, drink or smoke when using this product. P330:Rinse mouth. P203:Obtain, read and follow all safety instructions before use. P301+P316:IF SWALLOWED: Get emergency medical help immediately. P318:if exposed or concerned, get medical advice. P319:Get medical help if you feel unwell.

References

1. Mercer PF, Woodcock HV, Eley JD, Platé M, Sulikowski MG, Durrenberger PF, Franklin L, Nanthakumar CB, Man Y, Genovese F et al.. (2016) Exploration of a potent PI3 kinase/mTOR inhibitor as a novel anti-fibrotic agent in IPF.. Thorax, 71 (8): (701-11). [PMID:27103349] [10.1021/op500134e]

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Basic Description