Omipalisib (GSK-2126458)
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 205480

CAS#: 1086062-66-9

Description: Omipalisib, also known as GSK2126458, is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity. PI3K inhibitor GSK2126458 binds to and inhibits PI3K in the PI3K/mTOR signaling pathway, which may trigger the translocation of cytosolic Bax to the mitochondrial outer membrane, increasing mitochondrial membrane permeability and inducing apoptotic cell death. Bax is a member of the proapoptotic Bcl2 family of proteins. PI3K, often overexpressed in cancer cells, plays a crucial role in tumor cell regulation and survival.


Price and Availability

Size
Price

10mg
USD 150
100mg
USD 850
1g
USD 3250
Size
Price

25mg
USD 250
200mg
USD 1350
2g
USD 4850
Size
Price

50mg
USD 450
500mg
USD 2050
5g
Ask price

Omipalisib (GSK2126458), purity > 98%, is in stock. The same day shipping out after order is received. . Note: lead time for order > 100mg may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205480
Name: Omipalisib (GSK-2126458)
CAS#: 1086062-66-9
Chemical Formula: C25H17F2N5O3S
Exact Mass: 505.10202
Molecular Weight: 505.5
Elemental Analysis: C, 59.40; H, 3.39; F, 7.52; N, 13.85; O, 9.50; S, 6.34


Synonym: GSK2126458; GSK-2126458; GSK 2126458; Omipalisib

IUPAC/Chemical Name: 2,4-difluoro-N-(2-methoxy-5-(4-(pyridazin-4-yl)quinolin-6-yl)pyridin-3-yl)benzenesulfonamide

InChi Key: CGBJSGAELGCMKE-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: O=S(C1=CC=C(F)C=C1F)(NC2=CC(C3=CC=C4N=CC=C(C5=CC=NN=C5)C4=C3)=CN=C2OC)=O


Technical Data

Appearance:
light yellow solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

GSK2126458 is a highly potent PI3K and mTOR inhibitor. In vivo, GSK2126458 showed anti-tumor activity in both pharmacodynamic and tumor growth efficacy models. GSK2126458 reduced the phosphorylated AKT, p70S6K contents in a dose and time dependent way. The IC50 of GSK2126458 is 2 nM for pAKT in the HCC1954 breast carcinoma cell line. In various human tumor cells, GSK2126458 had a width of inhibitory activity for potent cell growth and induced cell death. Notably, GSK2126458 acted mainly by not induction of apoptosis but cell cycle arrest, particularly in G1-phase 
  


References