(-)-TK216

(-)-TK216 is an enantiomer of TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. (-)-TK216 has anti-cancer activity.

Product information

CAS Number: 1903783-78-7

Molecular Weight: 376.23

Formula: C19H15Cl2NO3

Chemical Name: 4,7-dichloro-3-[2-(4-cyclopropylphenyl)-2-oxoethyl]-3-hydroxy-2,3-dihydro-1H-indol-2-one

Smiles: OC1(CC(=O)C2C=CC(=CC=2)C2CC2)C2=C(NC1=O)C(Cl)=CC=C2Cl

InChiKey: ZWHNLSHDLKIXOG-UHFFFAOYSA-N

InChi: InChI=1S/C19H15Cl2NO3/c20-13-7-8-14(21)17-16(13)19(25,18(24)22-17)9-15(23)12-5-3-11(4-6-12)10-1-2-10/h3-8,10,25H,1-2,9H2,(H,22,24)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (265.79 mM; Need ultrasonic).

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:

(-)-TK216 (compound 14; for 3 days) has an IC50<5 μM in SKES cells (Ewing Sarcoma cell line). (-)-TK216 has T1/2s of 27.7 mins, 2.8 mins, 23.1 mins and 40.8 mins for human, rat, mouse, dog liver microsomes.

In Vivo:

(-)-TK216 (compound 14; 5 mg/kg for iv or 25 mg/kg for po) has T1/2s of 0.8 hours and 3.1 hours, and AUCs of 4131 h•(ng/mL) and 13152 h•(ng/mL) for iv and po, respectively, in BALB/c mice or Sprague Dawley rats.

Products are for research use only. Not for human use.