SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC 50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity In Vitro SIAIS178 (1-100 nM; for 16 hours) significantly reduces the BCR-ABL protein levels in a concentration dependent manner. SIAIS178 significantly inhibits the phosphorylation of BCR-ABL and the substrates STAT5. SIAIS178 (1, 10, 100, 1000 nM) exerts significant antiproliferative activity in BCR-ABL driven CML cell lines. SIAIS178 retains potency and selectivity against the BCR-ABL driven cell lines. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: K562 cells Concentration: 1, 3, 10, 30, 100 nM Incubation Time: 16 hours Result: Significantly reduced the BCR-ABL protein levels in a concentration dependent manner. In Vivo SIAIS178 (ip; 5, 15, and 45 mg/kg; 12 days) attenuates tumor progression in a dose-dependent manner, as determined by serial volumetric measurement . SIAIS178 (iv or ip; 2 mg/kg; 24 hours) has T 1/2 of 3.82 and 12.35 hours and C max of 1165.2 nM and 30 nM for iv and ip, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NOD/SCID mice with termed K562-Luc Dosage: 5, 15, and 45 mg/kg Administration: Ip; 12 days Result: Attenuated tumor progression in a dose-dependent manner, as determined by serial volumetric measurement. Animal Model: Female Wistar rats Dosage: 2 mg/kg (Pharmacokinetic Analysis) Administration: Iv or ip; 24 hours Result: Had T 1/2 of 3.82 and 12.35 hours and C max of 1165.2 nM and 30 nM for iv and ip, respectively. IC50& Target:VHL Bcr-Abl 24 nM (IC 50 )
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SIAIS178
CAS number：2376047-73-1(DMSO) molecular formula：C50H62ClN11O6S2
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2376047-73-1(DMSO) | molecular formula | C50H62ClN11O6S2 |
| molecular weight | 1012.68 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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