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SML4252

AR/AR-V7 degrader 27c

≥98% (HPLC), powder, E3 ligase inducer

Synonym(s):

4-(3-(2-((8-Fluoroquinolin-5-yl)amino)ethyl)-4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile

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About This Item

Empirical Formula (Hill Notation):
C24H19F4N5O2
CAS Number:
2841308-96-9
Molecular Weight:
485.43
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

SMILES string

N#CC1=CC=C(N2C(N(CCNC3=C4C=CC=NC4=C(C=C3)F)C(C)(C)C2=O)=O)C=C1C(F)(F)F

Biochem/physiol Actions

Compound 27c (cpd 27c) is a potent and selective inducer of E3 ligase MDM2-mediated degradation of androgen receptor (AR) and the constitutively active splice variant AR-V7 (DC50 = 2.67 and 2.64 μM, respectively, post 24h treatment in 22RV1 cells). Cpd 27c selectively inhibits AR-dependent proliferation in prostate cancer cultures (IC50 = 0.9 μM/22RV1 and 1.4 μM/LNCaP, >50 μM/AR-neg DU-145) and exhibits antitumor efficacy in an enzalutamide-resistant 22RV1 xenograft model in mice in vivo (10 or 30 mg/kg vial daily i.v.) by suppressing AR signaling pathway transcriptional activity.

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302

Hazard Classifications

Acute Tox. 4 Oral

Storage Class

10 - Combustible liquids

flash_point_f

Not applicable

flash_point_c

Not applicable

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