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ER degrader 10

CAT: 0804-HY-170377Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-170377Size:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
ER degrader 10 (Compound 51) is a selective, orally active degrader and antagonist for estrogen receptor (ER) with a DC50 of 0.43 nM and an IC50 of 0.56 nM. ER degrader 10 inhibits the proliferation of ER-positive cells with IC50s of 0-15 nM. ER degrader 10 exhibits a weak inhibitory activity against hERG channel with an IC50 >40 μM. ER degrader 10 is blood-brain barrier penetrable with a brain/plasma ratio (Kp) of 3.05. ER degrader 10 exhibits antitumor efficacy in mice model[1].
CAS Number
3035311-43-1
UNSPSC
12352100
Target
Estrogen Receptor/ERR; Potassium Channel
Related Pathways
Membrane Transporter/Ion Channel; Vitamin D Related/Nuclear Receptor
Field of Research
Cancer
Smiles
FC(C=C1)=CC(OC)=C1[C@H]2CSC3=CC(O)=CC=C3[C@H]2C4=CC=C(OCCN5CC(CF)C5)C=C4
Molecular Formula
C28H29F2NO3S
Molecular Weight
497.60
References & Citations
[1]Zhang D, et al., Discovery of Thiochroman Derivatives as Potent, Oral Selective Estrogen Receptor Degraders and Antagonists for the Treatment of Endocrine-Resistant Breast Cancer. J Med Chem. 2024 Dec 12;67 (23) :21545-21567.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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