SIAIS178 - 10mM in DMSO , CAS No.2376047-73-1

CAS: 2376047-73-1 Cat. No.: S655436 분자식: C₅₀H₆₂ClN₁₁O₆S₂ 분자량: 1012.68 PubChem CID: 139474625

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

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 )

Specifications

사양 및 순도

10mM in DMSO

생화학 및 생리적 메커니즘

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

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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이름과 식별자

• 이성체 SMILES: CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)C(=O)CCCCCCC(=O)N[C@H](C(=O)N5C[C@@H](C[C@H]5C(=O)NCC6=CC=C(C=C6)C7=C(N=CS7)C)O)C(C)(C)C
• PubChem CID: 139474625
• 분자량: 1012.68

자주 묻는 질문

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2376047-73-1, the molecular formula is C50H62ClN11O6S2, and the molecular weight is 1012.68 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.