gdc-0927-racemate

Description: GDC-0927 Racemate, the racemic mixture of GDC-0927, is used in the research of ER-related diseases. GDC-0927 (formerly known as SRN-927) is a degrader of estrogen receptor (SERD) that potently inhibits ER-alpha activity with an IC50 of 0.2 nM. As a novel, potent, non-steroidal, orally bioavailable, selective ER (estrogen receptor)antagonist/ER degrader (SERD), GDC-0927 induces tumor regression in ER+ BC patient-derived xenograft models. GDC-0927 appears well-tolerated to date with PK exposure supporting QD dosing, evidence of robust PD target engagement, and encouraging anti-tumor activity in heavily pretreated pts with advanced or metastatic ER+ BC, including pts with ESR1 mutations. GDC-0927 is a next-generation orally active SERD which appears to have greater potential than GDC-0810 to be a best-in-class SERD molecule. GDC-0927 targets estrogen receptor alpha (ERalpha), a receptor expressed in more than 70% of breast cancers, making it a popular target for the disease.

References: AACR; Cancer Res 2018; 78(4 Suppl):Abstract nr PD5-10.

Related CAS#:1642297-01-5 (free base); 1642297-02-6 (HCl); 1642297-03-7 (HBr)