Product Name :
ERα degrader-2
Description:
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 druggability, can be used for HER+ breast cancer research.
CAS:
2235396-63-9
Molecular Weight:
492.53
Formula:
C29H27F3N2O2
Chemical Name:
3′, 5′-difluoro-4′-[(1R, 3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1H, 2H, 3H, 4H, 9H-pyrido[3, 4-b]indol-1-yl]-[1, 1′-biphenyl]-4-carboxylic acid
Smiles :
C[C@@H]1CC2=C(NC3=CC=CC=C32)[C@@H](C2C(F)=CC(=CC=2F)C2C=CC(=CC=2)C(O)=O)N1CC(C)(C)F
InChiKey:
XKYAKCQZMYWSSE-CHAGWJKLSA-N
InChi :
InChI=1S/C29H27F3N2O2/c1-16-12-21-20-6-4-5-7-24(20)33-26(21)27(34(16)15-29(2,3)32)25-22(30)13-19(14-23(25)31)17-8-10-18(11-9-17)28(35)36/h4-11,13-14,16,27,33H,12,15H2,1-3H3,(H,35,36)/t16-,27-/m1/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.NLRP1 Protein, Human custom synthesis
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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 druggability, can be used for HER+ breast cancer research.|Product information|CAS Number: 2235396-63-9|Molecular Weight: 492.53|Formula: C29H27F3N2O2|Chemical Name: 3′, 5′-difluoro-4′-[(1R, 3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1H, 2H, 3H, 4H, 9H-pyrido[3, 4-b]indol-1-yl]-[1, 1′-biphenyl]-4-carboxylic acid|Smiles: C[C@@H]1CC2=C(NC3=CC=CC=C32)[C@@H](C2C(F)=CC(=CC=2F)C2C=CC(=CC=2)C(O)=O)N1CC(C)(C)F|InChiKey: XKYAKCQZMYWSSE-CHAGWJKLSA-N|InChi: InChI=1S/C29H27F3N2O2/c1-16-12-21-20-6-4-5-7-24(20)33-26(21)27(34(16)15-29(2,3)32)25-22(30)13-19(14-23(25)31)17-8-10-18(11-9-17)28(35)36/h4-11,13-14,16,27,33H,12,15H2,1-3H3,(H,35,36)/t16-,27-/m1/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.Malonyl CoA manufacturer |Shelf Life: ≥12 months if stored properly.PMID:31613496 |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|ERα degrader-2 (0.01-40 nM) decreases ERα expression and not fully degrades ERα in MCF-7 cells even at a higher biochemical concentration in MCF7 cells.|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. ERα degrader-2 (oral gavage; 2 mg/kg; single dose) possesses better pharmacokinetic properties than AZD9496, 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%.|Products are for research use only. Not for human use.|
