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[1,1'-Biphenyl]-4-carboxylic acid, 3',5'-difluoro-4'-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1H-pyrido[3,4-b]indol-1-yl]- manufacturers
- ERα degrader-2
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- $199.00
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2026-07-27
- CAS:2235396-63-9
- Purity: 99.71%
- Supply Ability: 10g
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| | [1,1'-Biphenyl]-4-carboxylic acid, 3',5'-difluoro-4'-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1H-pyrido[3,4-b]indol-1-yl]- Basic information |
| Product Name: | [1,1'-Biphenyl]-4-carboxylic acid, 3',5'-difluoro-4'-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1H-pyrido[3,4-b]indol-1-yl]- | | Synonyms: | [1,1'-Biphenyl]-4-carboxylic acid, 3',5'-difluoro-4'-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1H-pyrido[3,4-b]indol-1-yl]-;ERα degrader-2 | | CAS: | 2235396-63-9 | | MF: | C29H27F3N2O2 | | MW: | 492.53 | | EINECS: | | | Product Categories: | | | Mol File: | 2235396-63-9.mol | ![[1,1'-Biphenyl]-4-carboxylic acid, 3',5'-difluoro-4'-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1H-pyrido[3,4-b]indol-1-yl]- Structure](CAS/20210305/GIF/2235396-63-9.gif) |
| | [1,1'-Biphenyl]-4-carboxylic acid, 3',5'-difluoro-4'-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1H-pyrido[3,4-b]indol-1-yl]- Chemical Properties |
| Boiling point | 596.0±50.0 °C(Predicted) | | density | 1.275±0.06 g/cm3(Predicted) | | pka | 3.89±0.10(Predicted) | | form | Solid | | color | Brown to reddish brown |
| | [1,1'-Biphenyl]-4-carboxylic acid, 3',5'-difluoro-4'-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1H-pyrido[3,4-b]indol-1-yl]- Usage And Synthesis |
| Uses | ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER+ breast cancer research[1]. | | in vivo | ERα degrader-2 (oral administration; 2-6 mg/kg; QD; 21 days) leads to the significant tumor growth inhibition and decreases tumor volume in mice[1].ERα degrader-2 (oral gavage; 2 mg/kg; single dose) possesses better pharmacokinetic properties thanAZD9496, the plasma exposure (AUC) is 16073.7 h*ng/mL, and the half-life period is 12.1 h, the oral availability is 80.5%[1]. | Animal Model: | MCF-7 human breast cancer xenograft model in nude mice[1] | | Dosage: | 2 mg/kg; 6 mg/kg | | Administration: | Oral administration; 2-6 mg/kg; QD; 21 days | | Result: | Exhibited in vivo efficacy in breast cancer xenograft model. |
| | IC 50 | ERα: 4.6 nM (IC50) | | References | [1] Xiaomeng Zhang, et al. Dynamics-Based Discovery of Novel, Potent Benzoic Acid Derivatives as Orally Bioavailable Selective Estrogen Receptor Degraders for ERα+ Breast Cancer. J Med Chem DOI:10.1021/acs.jmedchem.1c00280 |
| | [1,1'-Biphenyl]-4-carboxylic acid, 3',5'-difluoro-4'-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1H-pyrido[3,4-b]indol-1-yl]- Preparation Products And Raw materials |
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