JB170 - ≥98% , CAS No.2705844-82-0

CAS: 2705844-82-0 Cat. No.: J647029 分子式: C₄₈H₄₄ClFN₈O₁₁ 分子量: 963.36

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Application

PROTAC

概要

JB170 is a potent and highly specific PROTAC -mediated AURORA-A ( Aurora Kinase ) degrader ( DC 50 =28 nM) by linking Alisertib, to the Cereblon -binding molecule Thalidomide. JB170 preferentially binds AURORA-A ( EC 50 =193 nM) over AURORA-B (EC 50 =1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase

In Vitro

JB170 (1 μM; 24-72 hours; MV4-11 cells) mediates Aurora-A depletion inhibiting cancer cell survival. ?\nJB170 (0.01-10 μM; 6 hours; MV4-11 cells) reduces AURORA-A levels. ?\nJB170 (0.5 μM; 12 hours; MV4-11 cells) delays/arrests S-phase progression. ?\nJB170 (0.5 μM; 0-72 hours; MV4-11 cells) induces apoptosis is exclusively caused by targeting AURORA-A. ?\nJB170 (0.1 μM; 0-9 hours; IMR5 cells) shows rapid AURORA-A depletion. JB170 (0~1 μM; 6 hours; MV4-11 cells) strongly attenuates in mutants with respect to AURORA-A. JB170 (0.1 μM; 18 hours; MV4-11 cells) does not activate AURORA-A. JB170 (0~1 μM; 24 hours; IMR5 cells) largely abrogates AURORA-A T217D depletion. JB170 (1 μM; 4 days; IMR5 cells) mediates Aurora-A depletion inhibiting cancer cell survival. JB170 (IMR5 cells) reduces AURORA-A levels by lowering AURORA-A mRNA levels. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MV4-11 cells Concentration: 1 µM Incubation Time: 24-72 hours Result: After 72 hours, the number of viable cells was 32% of control levels. Western Blot AnalysisCell Line: MV4-11 cells Concentration: 0.01~10 μM Incubation Time: 6 hours Result: Substantial degradation was observed at 100 nM and 1 µM. Apoptosis AnalysisCell Line: MV4-11 cells Concentration: 0.5 µM Incubation Time: 0~72 hours Result: Apoptosis was exclusively caused by targeting AURORA-A. Cell Cycle AnalysisCell Line: MV4-11 cells Concentration: 0.5 µM Incubation Time: 12 hours Result: Delayed or arrested S-phase progression.

Form:Solid

IC50& Target:Aurora A 28 nM (DC 50 ) Aurora A 99 nM (Kd) Aurora A 193 nM (EC 50 ) Cereblon

Specifications

仕様と純度

≥98%

生化学的・生理学的メカニズム

JB170 is a potent and highly specific PROTAC -mediated AURORA-A ( Aurora Kinase ) degrader ( DC 50 =28 nM) by linking Alisertib, to the Cereblon -binding molecule Thalidomide. JB170 preferentially binds AURORA-A ( EC 50 =193 nM) over AURORA-B (EC 50 =1.4

保管条件

Store at -20°C

入荷

Ice chest + Ice pads

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

アクションタイプ

INHIBITOR

純度

≥98%

名前と識別子

• 分子量: 963.36

化学的性質と物理的性質

• 溶解度: DMSO : 100 mg/mL (103.80 mM; Need ultrasonic)

よくある質問

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

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

The CAS Number is 2705844-82-0, the molecular formula is C48H44ClFN8O11, and the molecular weight is 963.36 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.