1. PROTAC
    Protein Tyrosine Kinase/RTK
  2. PROTAC
    Bcr-Abl
  3. SIAIS178

SIAIS178 

Cat. No.: HY-128756
Handling Instructions

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.

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SIAIS178 Chemical Structure

SIAIS178 Chemical Structure

CAS No. : 2376047-73-1

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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].

IC50 & Target[1]

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.
Molecular Weight

1012.68

Formula

C₅₀H₆₂ClN₁₁O₆S₂

CAS No.

2376047-73-1

SMILES

O=C(N1CCN(C2=NC(C)=NC(NC3=NC=C(C(NC4=C(C=CC=C4Cl)C)=O)S3)=C2)CC1)CCCCCCC(N[[email protected]@H](C(C)(C)C)C(N5[[email protected]@H](C[[email protected]@H](O)C5)C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

SIAIS178SIAIS 178SIAIS-178PROTACBcr-AblProteolysis-targeting chimeradegradationrecruitVonHippel-LindauVHLE3ubiquitinligaseanticanceractivityInhibitorinhibitorinhibit

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