NEO-811
NEO-811 is a selective and orally active ARNT (HIF-1β) molecular glue degrader. NEO-811 is mediated by CRL4-CRBN E3 ligase for ARNT degradation. NEO-811 can be used for the study of clear cell renal cell carcinoma (ccRCC).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 3084635-77-5
- 화학식: C30H30FN5O4
- 분자량:543.59
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
IC50 & Target
|
HIF-1β |
In Vitro
NEO-811 is highly selective and does not degrade well-known neosubstrates. Transcriptomic profiling of NEO-811 activity across several VHL-deficient ccRCC cell lines confirmed suppression of HIF-2α target genes, including cyclin D and vascular endothelial growth factor (VEGF). NEO-811 also uniquely suppresses expression of target genes regulated by other Class I bHLH-PAS transcription factors, including HIF-1α and aryl hydrocarbon receptor (AHR). NEO-811 retaines activity in HIF-2α inhibitor-resistant cells that harbored previously described mutations[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 3084635-77-5
-
분자량 543.59
-
화학식 C30H30FN5O4
-
SMILES
O=C1CCC(C2=CN=C(C=CC([C@@]3(O)CCN(CC4=CC=C(C5=NOC=N5)C=C4)CC3(C)C)=C6F)C6=C2)C(N1)=O
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)