Products

Enzymes for Research, Diagnostic and Industrial Use

GDC-0032

Cat No.
CEI-0867
Description
GDC-0032 is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with IC50 of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over β.
Alias
RG7604
CAS No.
1282512-48-4
Molecular Weight
460.53
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
Synonyms
RG7604
Targets
PI3Kα, PI3K β, PI3K δ, PI3Kγ
IC50
0.29 nM; 9.1 nM; 0.12 nM; 0.97 nM
Molecular Formula
C24H28N8O2
Chemical Name
1H-Pyrazole-1-acetamide, 4-[5,6-dihydro-2-[3-methyl-1-(1-methylethyl)-1H-1,2,4-triazol-5-yl]imidazo[1,2-d][1,4]benzoxazepin-9-yl]-α,α-dimethyl-
Solubility
DMSO mg/mL; Water mg/mL; Ethanol mg/mL
In vitro
GDC-0032 is an orally bioavailable, potent, and selective inhibitor of Class I PI3Kα, δ, and γ isoforms, with 30 fold less inhibition of the PI3K β isoform relative to the PI3Kα isoform. Preclinical data show that GDC-0032 has increased activity against PI3Kα isoform (PIK3CA) mutant and HER2-amplified cancer cell lines. GDC-0032 inhibits MCF7-neo/HER2 cells proliferation with IC50 of 2.5 nM.
In vivo
GDC-0032 pharmacokinetics is approximately dose proportional and time independent with a mean t1/2 of 40 hours. The combination of GDC-0032 enhances activity of fulvestrant resulting in tumor regressions and tumor growth delay (91% tumor growth inhibition (TGI)). In addition, the combination of GDC-0032 with tamoxifen enhances the efficacy of tamoxifen in vivo (102%TGI for GDC-0032).
Download Datasheet:



Inquiry
Realted Products
Catalog
ProductName
EC No.
CAS No.
Source
Price
CatalogCEI-0078
ProductNameCAY10505
EC No.
CAS No.1218777-13-9
Source
CatalogCEI-0080
ProductNameAS-605240
EC No.
CAS No.648450-29-7
Source
CatalogCEI-0088
ProductNameAS-252424
EC No.
CAS No.900515-16-4
Source
CatalogCEI-0091
ProductNamePIK-90
EC No.
CAS No.677338-12-4
Source
+ See More >>
Online Inquiry
Name:
*Phone:
*E-mail Address:
Country:
Company/Institution:
*Products or Services Interested:
Quantity:
Project Description:
Our Products are Not Intended for Private Therapeutic Use!
*Verification Code:
Please input "enzymes"(case insensitive) as verification code.

Welcome! For price inquiries, please feel free to contact us through the form below through the form on the left side. We will get back to you as soon as possible.

Sitemap  Privacy Policy
Copyright ©2011 - 2017 Creative Enzymes.
Contact Us 45-1 Ramsey Road, Shirley, NY 11967, USA
Email: info@creative-enzymes.com
Tel: 1-631-562-8517 1-631-448-7888
Fax: 1-631-938-8127
Distributors To view the contact information for a specific location, select the desired country: