CH5132799 Inhibitor CAS No. 1007207-67-1

Cat. No.	Name	Size	Price
KI0600	CH5132799	10 mg	$592
	CH5132799	50 mg	$1560
	CH5132799	100 mg	$2500
	CH5132799	200 mg	$3780

Chemical Characteristic

Product Name	CH5132799
CAS No.	1007207-67-1
Molecular Weight	377.42
Formula	C₁₅H₁₉N₇O₃S
Chemical Name	[5-[7-Methylsulfonyl-2-(morpholin-4-yl)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-yl]amine
Smiles	Nc1ncc(cn1)c1c2c(nc(n1)N1CCOCC1)N(CC2)S(=O)(=O)C
Chemical Structure

Biological activities

CH5132799 potently and selectively inhibits PI3Kα and mTOR with IC50 values of 14 nM and 1.6 µM, respectively. The IC50 values of CH5132799 are 120, 500, and 36 nM against PI3Kβ, PI3Kδ, and PI3Kγ, respectively. No significant inhibitory activities of CH5132799 are observed against a representative panel of 26 protein kinases, including RTKs, nonreceptor tyrosine kinases, and serine/threonine kinases. In vitro, CH5132799 shows strong antiproliferative activity against breast, ovarian, prostate, and endo-metrial cancer cells in which the PI3K pathway is often activated. In vitro, cancer cell lines harboring PIK3CA mutations are significantly sensitive to CH5132799.^[1] In human tumor cell lines with PI3K pathway activation, CH5132799 shows potent antiproliferative activity. CH5132799 is orally available. and CH5132799 has significant antitumor activity in PI3K pathway-activated human cancer xenograft models in mice.^[2] In vivo, CH5132799 administrations also have potent antitumor activity in xenograft models with PIK3CA mutations.^[1]

References

[1] Tanaka H, et al. The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011, 17(10): 3272-3281. [2] Ohwada J. Nielsen, et al. Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorg Med Chem Lett. 2011, 21(6): 1767-1772.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com