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ACBI2 is a highly potent and orally active VHL PROTAC SMARCA2 degrader (EC50: 7?nM), which selectively degrades SMARCA2 with a DC50 value of 1?nM in RKO cells. ACBI2 can be used in the research of lung cancer[1]. | [in vivo]
ACBI2 (80?mg/kg, p.o., once daily) significantly inhibits tumor growth in an A549 xenograft mice model[1].
ACBI2 (5-100 mg/kg, p.o., tumors collected 24 or 48?h after treatment) dose-dependently degrades tumor SMARCA2 in A549 engrafted tumor bearing mice (IHC staining)[1].
ACBI2 (30 mg/kg, p.o., mice) shows oral bioavailability of 22%[1].
| Animal Model: | A549 xenograft mice model[1] | | Dosage: | 80?mg/kg | | Administration: | Oral administration (p.o.), once daily | | Result: | Inhibited tumor growth and was well tolerated. |
| [IC 50]
VHL: 7 nM (EC50); SMARCA2 | [References]
[1] Kofink C, et al. A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo. Nat Commun. 2022 Oct 10;13(1):5969. DOI:10.1038/s41467-022-33430-6 |
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| Company Name: |
TargetMol
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| Telephone: |
400-821-0310 15002144251 |
| Website: |
www.targetmol.cn/ |
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