SIAIS178

SKU: orb1708526

Description

SIAIS178 is a potent and selective PROTAC molecule that targets BCR-ABL for degradation via recruitment of the VHL E3 ligase, with an IC50 of 24 nM. It demonstrates robust anti-proliferative activity in leukemia cell cultures and has been shown to induce regression in K562 xenograft tumor models in vivo.

Research Area

Cardiovascular Research, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 2376047-73-1
• MW: 1012.68
• Purity: 98.07% (May vary between batches)
• Formula: C₅₀H₆₂ClN₁₁O₆S₂
• SMILES: C([C@@H](NC(CCCCCCC(=O)N1CCN(CC1)C=2C=C(NC=3SC(C(NC4=C(C)C=CC=C4Cl)=O)=CN3)N=C(C)N2)=O)[C@](C)(C)C)(=O)N5[C@H](C(NCC6=CC=C(C=C6)C7=C(C)N=CS7)=O)C[C@@H](O)C5
• Target: Ligands for E3 Ligase,Bcr-Abl,PROTACs
• Solubility: DMSO:245 mg/mL (241.93 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (4.94 mM)

Bioactivity

• Target IC50:
  VHL:24 nM|BCR-ABL:24 nM
• In Vivo:
  Methods: SIAIS178 (5, 15, and 45 mg/kg) was used to treat K562-Luc NOD/SCID mice and investigate its effect on tumor progression in vivo. Results: SIAIS178 attenuated tumor progression in a dose-dependent manner as determined by serial volume measurements.
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• In Vitro:
  Methods: K562 cells were treated with SIAIS178 (1, 3, 10, 30, 100 nM, 16 hours) and BCR-ABL protein expression was detected by Western blot. Results: SIAIS178 significantly reduced BCR-ABL protein levels in a concentration-dependent manner.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BcrAbl, Bcr-Abl, SIAIS 178, SIAIS178, SIAIS-178, SIAI S178, VHL

Compound Identifiers

PubChem CID

139474625