Fig. 1 · Structure

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SR-2211

Cat. No. A13568 CAS 1359164-11-6

RORγ Antagonist

SR-2211 selectively binds RORr(Ki = 105 nM), acting as an inverse agonist of constitutive in vitro RORr activity (IC50 = 320 nM).

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
CWR22R IC50 10.13 μM Antiproliferative activity against human 22Rv1 cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay [PMID: 34121397]
CWR22R IC50 6.42 μM Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by celltiter-glo assay [PMID: 30964293]
DU-145 IC50 45.69 μM Antiproliferative activity against human DU145 cells measured after 72 hrs by celltiter-glo assay [PMID: 30964293]
HEK293 EC50 320 nM Agonist activity at RoRc-LBD (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 reporter assay [PMID: 24502334]
HEK-293T IC50 0.11 μM Inhibition of Gal4-RORgamma-LBD (180 to 507 residues) (unknown origin) expressed in HEK293T cells after 24 hrs by dual-luciferase reporter assay [PMID: 27043267]
HEK-293T IC50 320 nM Inhibition of GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells assessed as suppression of transcriptional activity after 20 hrs 10.1039/C3MD00005B
HepG2 IC50 150 nM Displacement of [3H]T0901317 from human RoRc expressed in HepG2 cells by scintillation proximity binding assay [PMID: 24502334]
LNCaP IC50 5.38 μM Antiproliferative activity against human LNCaP cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay [PMID: 34121397]
LNCaP IC50 6.79 μM Antiproliferative activity against human LNCAP cells measured after 96 hrs by celltiter-glo assay [PMID: 30964293]
LNCaP C4-2B IC50 10.06 μM Antiproliferative activity against human C4-2B cells measured after 96 hrs by celltiter-glo assay [PMID: 30964293]
LNCaP C4-2B IC50 5.38 μM Antiproliferative activity against human LNCaP C4-2B cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay [PMID: 34121397]
PC-3 IC50 24.82 μM Antiproliferative activity against human PC3 cells measured after 72 hrs by celltiter-glo assay [PMID: 30964293]

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Specifications

Manufacturer Adooq Bioscience
Actions Agonist
CAS Number 1359164-11-6
Applications RORγ Antagonist
Formula C26H24F7N3O
Molecular Weight 527.5
SMILES
C1CN(CCN1CC2=CC=C(C=C2)C3=C(C=C(C=C3)C(C(F)(F)F)(C(F)(F)F)O)F)CC4=CC=NC=C4

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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