GNE-149 is an orally bioavailable full antagonist of estrogen receptor α ( ERα ; IC 50 =0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancerIn VitroGNE-149 exhibits antiproliferative activity in MCF7 and T47D cells with IC 50 s of 0.66 and 0.69 nM, respectively. GNE-149 exhibits ERα Degradation in MCF7 and T47D cells with IC 50 s of 0.053 and 0.031 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoGNE-149 (0.3-30 mg/kg) exhibits in vivo efficacy in an MCF7 xenograft mouse model harboring either wild-type (WT) ERα or overexpressed Y537S mutant . GNE-149 has favorable pharmacokinetic profile, including total clearance (CL; 19, 8, and 13 mL/min/kg for Rat, Dog, and Cyno) and oral bioavailability (F; 31%, 49%, and 28% for Rat, Dog, and Cyno) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female Crl:NU Foxn1 nu mice (at 7 weeks of age) bearing wild-type (WT) ERαor overexpressed Y537S mutant MCF7 tumor Dosage: 0.3, 1, 3, 10, and 30 mg/kg Administration: Orally q.d. for 21 days Result: Exhibited dose-dependent efficacy in the MCF7 WT and Y537S mutant xenograft model, with tumor regression observed at all doses above 0.3 mg/kg in Y537S mutant xenograft model.Form:SolidIC50& Target:ERα 0.053 nM (IC 50 ). Specification: 0.99 Molecular Formula: C28H33F4N3O Molecular Weight: 503.57 PubChem CID: 121410669 Isomeric SMILES: C[C@@H]1CC2=C([C@H](N1CC(C)(C)F)C3=C(C=C(C=C3F)OC4CN(C4)CCCF)F)NC5=CC=CC=C25
- UPC:
- 51184005
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 1.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- G648993-5mg
- CAS:
- 1953132-75-6
- Product Size:
- 5mg
