Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
8 Results for "
Y537S mutat
" in MedChemExpress (MCE) Product Catalog:
Products (8)
8 Results for "Y537S mutat" in MCE Product Catalog:
7
7 Cited Publications
Synonyms: GDC-9545; RG6171
Target:
Research Areas:
Giredestrant (GDC-9545) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant promotes the degradation of ERα protein, including the ESR1 Y537S mutant ERα. Giredestrant reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant induces tumor regression in both ESR1 Y537S mutant and wild-type ERα tumor models. Giredestrant can be used for the research of ER + breast cancer .
Cat. No.: HY-145071
CAS No.: 2667598-05-0
Target:
Research Areas:
PROTAC ERα Y537S degrader-1 comprises a ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Y537S degrader-1 extracts from patent WO2021143822, example 12. PROTAC ERα Y537S degrader-1 is an estrogen receptor-alpha (ERα) Y537S degrader .
Cat. No.: HY-135903
CAS No.: 2407529-33-1
Synonyms: GDC-9545 tartrate; RG6171 tartrate
Target:
Giredestrant tartrate (GDC-9545 tartrate) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant tartrate promotes the degradation of ERα protein, including the ESR1 Y537S mutant ERα. Giredestrant tartrate reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant tartrate induces tumor regression in both ESR1 Y537S mutant and wild-type ERα tumor models. Giredestrant tartrate can be used for the research of ER + breast cancer .
Cat. No.: HY-101119
CAS No.: 2077980-80-2
Target:
Research Areas:
GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC50=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.
Cat. No.: HY-164924
CAS No.: 3026007-23-5
Target:
Research Areas:
ERD-12310A is an orally active ERα PROTAC degrader, with a Ki value of 0.95 nM against human ERα and a DC50 of 47 pM for ERα in MCF-7 cells. ERD-12310A forms a ternary complex with ERα and the CRBN E3 ubiquitin ligase, thereby inducing ubiquitination and proteasomal degradation of wild-type and ESR1 Y537S mutant ERα. ERD-12310A induces tumor regression in ER+ breast cancer xenografts and inhibits tumor growth in ESR1 Y537S mutant breast cancer xenografts. ERD-12310A can be used in studies related to ER-positive breast cancer and ESR1-mutant breast cancer .
Cat. No.: HY-109176R
CAS No.: 1953133-47-5
Synonyms: GDC-9545 (Standard); RG6171 (Standard)
Research Areas:
Giredestrant (Standard) (GDC-9545 (Standard); RG6171 (Standard)) is the analytical standard of Giredestrant (HY-109176). This product is intended for research and analytical applications. Giredestrant (GDC-9545) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant promotes the degradation of ERα protein, including the ESR1 Y537S mutant ERα. Giredestrant reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant induces tumor regression in both ESR1 Y537S mutant and wild-type ERα tumor models. Giredestrant can be used for the research of ER + breast cancer .
Cat. No.: HY-179510
Target:
Research Areas:
CDD-1274 is an ERα (Estrogen receptor α) variant inhibitor. CDD-1274 induces proteasomal degradation of ERα variants in breast cancer cell lines and causes Y537S ERα degradation. CDD-1274 potently blocks ligand-dependent and ligand-independent ER signaling in endocrine-resistant breast cancer cells. CDD-1274 can be used for the study of breast cancer .
Cat. No.: HY-184982
Estrogen receptor-IN-2 is a potent estrogen receptor inhibitor formed by the conjugation of Tam (HY-13757)-NHC and gold (I). Estrogen receptor-IN-2 significantly downregulates estrogen receptor (ER) levels, inhibits ER-mediated downstream signaling pathways, and induces immunogenic cell death (ICD) mediated by damage-associated molecular patterns (DAMPs). Estrogen receptor-IN-2 can overcome drug resistance in MCF-7 Y537S mutant cells via the RAMP3/CALCR signaling pathway. It is suitable for research on endocrine-resistant breast cancer .
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
