1086062-66-9 | Gsk2126458

Packsize	Purity	Availability	Price	Discounted Price
1mg	95%	in stock	$48.00	$34.00
2mg	95%	in stock	$67.00	$47.00
5mg	95%	in stock	$108.00	$76.00
10mg	95%	in stock	$159.00	$111.00
25mg	95%	in stock	$322.00	$225.00
100mg	95%	in stock	$348.00	$244.00
250mg	95%	in stock	$581.00	$407.00
1g	95%	in stock	$1,536.00	$1,075.00

Description

• Catalog Number: AE11234
• Chemical Name: Gsk2126458
• CAS Number: 1086062-66-9
• Molecular Formula: C25H17F2N5O3S
• Molecular Weight: 505.496
• MDL Number: MFCD16038929
• SMILES: COc1ncc(cc1NS(=O)(=O)c1ccc(cc1F)F)c1ccc2c(c1)c(ccn2)c1ccnnc1

Computed Properties

• Complexity: 833
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 36
• Hydrogen Bond Acceptor Count: 10
• Hydrogen Bond Donor Count: 1
• Rotatable Bond Count: 6
• XLogP3: 3.3

Upstream Synthesis Route

Omipalisib is a potent and selective inhibitor of phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (PIK3CA), a key enzyme involved in the PI3K/AKT/mTOR signaling pathway. This pathway plays a crucial role in regulating cell growth, proliferation, and survival, making it a promising target for cancer therapy. In the realm of chemical synthesis, Omipalisib's unique mechanism of action can be leveraged to selectively inhibit the PI3K pathway in cancer cells, potentially leading to the development of novel anticancer agents. By modulating this signaling pathway, Omipalisib has the potential to impact various cellular processes that are critically involved in tumorigenesis, offering new avenues for the design and synthesis of targeted chemotherapeutic agents.

Literature

• Exploration of a potent PI3 kinase/mTOR inhibitor as a novel anti-fibrotic agent in IPF.

  Thorax 20160801

• Identification of potent Yes1 kinase inhibitors using a library screening approach.

  Bioorganic & medicinal chemistry letters 20130801

• Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20120815

• [11C]GSK2126458 and [18F]GSK2126458, the first radiosynthesis of new potential PET agents for imaging of PI3K and mTOR in cancers.

  Bioorganic & medicinal chemistry letters 20120215

• Comparison of the effects of the PI3K/mTOR inhibitors NVP-BEZ235 and GSK2126458 on tamoxifen-resistant breast cancer cells.

  Cancer biology & therapy 20110601

• Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin.

  ACS medicinal chemistry letters 20100408