Description
PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to CRBN E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells.
Product information
CAS Number: 2488851-89-2
Molecular Weight: 966.80
Formula: C40H53BrFN9O13
Chemical Name: (Z)-N-(3-bromo-4-fluorophenyl)-4-(27-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}-7,10,13,16,19,22,25-heptaoxa-1,4-diazaheptacosan-1-yl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
Smiles: O/N=C(\NC1C=CC(F)=C(Br)C=1)/C1=NON=C1NCCNCCOCCOCCOCCOCCOCCOCCOCCNC1C=CC=C2C=1C(=O)N(C1CCC(=O)NC1=O)C2=O
InChiKey: BVQZWOPTIZSOAW-UHFFFAOYSA-N
InChi: InChI=1S/C40H53BrFN9O13/c41-29-26-27(4-5-30(29)42)46-37(48-56)35-36(50-64-49-35)45-9-8-43-10-12-57-14-16-59-18-20-61-22-24-63-25-23-62-21-19-60-17-15-58-13-11-44-31-3-1-2-28-34(31)40(55)51(39(28)54)32-6-7-33(52)47-38(32)53/h1-5,26,32,43-44,56H,6-25H2,(H,45,50)(H,46,48)(H,47,52,53)
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.
Shelf Life: ≥12 months if stored properly.
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:
PROTAC IDO1 Degrader-1 (compound 2c) (10 μM; 24 hours) notably decreases IDO1 level induced by IFN-γ. PROTAC IDO1 Degrader-1 and IFN-γ (5 ng/mL) are incubated with HeLa cells for 24 h, and a significant dose-dependent degradation is observed. PROTAC IDO1 Degrader-1 combined with chimeric antigen receptor-modified T (CAR-T) cells can improve the tumor-killing activity of HER-2 CAR-T cells. PROTAC IDO1 Degrader-1 induces significant and persistent degradation of IDO1 with maximum degradation (dmax) of 93% in HeLa cells.
Products are for research use only. Not for human use.
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