2376047-73-1
2376047-73-1 structure
- Name: SIAIS178
- Chemical Name: SIAIS178
- CAS Number: 2376047-73-1
- Molecular Formula: C50H62ClN11O6S2
- Molecular Weight: 1012.68
- Catalog: Signaling Pathways PROTAC PROTAC
- Create Date: 2020-01-23 13:35:51
- Modify Date: 2024-01-09 17:24:37
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SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity[1].
| Name | SIAIS178 |
|---|
| Description | SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity[1]. |
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| Related Catalog | |
| Target |
VHL Bcr-Abl:24 nM (IC50) |
| 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[1]. 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[1]. Western Blot Analysis[1] Cell 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 [1]. SIAIS178 (iv or ip; 2 mg/kg; 24 hours) has T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively[1]. Animal Model: NOD/SCID mice with termed K562-Luc[1] 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[1] Dosage: 2 mg/kg (Pharmacokinetic Analysis) Administration: Iv or ip; 24 hours Result: Had T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively. |
| References |
| Molecular Formula | C50H62ClN11O6S2 |
|---|---|
| Molecular Weight | 1012.68 |
| Hazard Codes | Xi |
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