Tucatinib hemiethanolate - ≥99% , CAS No.1429755-56-5

CAS: 1429755-56-5 Cat. No.: T649673 分子式: C₂₆H₂₄N₈O₂.1/2C₂H₆O 分子量: 503.57 EC番号: 881-571-0 PubChem CID: 162623678

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

概要

Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC 50 of 8 nM.

In Vitro

Tucatinib hemiethanolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR. Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the EGFR overexpressing cell lines, it weakly inhibits phosphorylation and proliferation, demonstrating that Tucatinib may have potential to block HER2 signaling without causing the toxicities of EGFR inhibition. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tucatinib hemiethanolate (ONT-380 hemiethanolate, 200 mg/kg/d) shows a survival benefit when each drug is dosed at the maximum-tolerated dose . Tucatinib and its active metabolite causes a significant reduction in brain pErbB2 (80%). Tucatinib (ARRY-380) hemiethanolate demonstrates significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size) at the higher dose level in 9/12 animals. Tucatinib (50 mg/kg/d) in combination with trastuzumab shows a 98% TGI with complete regressions in 9/12 animals and two partial regressions. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female nude mice. Dosage: 200 mg/kg/d. Administration: PO, daily. Result: Exhibited anti-tumor activity and benefited survival.

Form:Solid

IC50& Target:IC50: 8 nM (HER2)

Specifications

仕様と純度

≥99%

生化学的・生理学的メカニズム

Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC 50 of 8 nM.

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。

純度

≥99%

名前と識別子

カノニカル・スマイル

CCO.CC1=C(C=CC(=C1)NC2=NC=NC3=C2C=C(C=C3)NC4=NC(CO4)(C)C)OC5=CC6=NC=NN6C=C5.CC1=C(C=CC(=C1)NC2=NC=NC3=C2C=C(C=C3)NC4=NC(CO4)(C)C)OC5=CC6=NC=NN6C=C5

異性体SMILES

CCO.CC1=C(C=CC(=C1)NC2=NC=NC3=C2C=C(C=C3)NC4=NC(CO4)(C)C)OC5=CC6=NC=NN6C=C5.CC1=C(C=CC(=C1)NC2=NC=NC3=C2C=C(C=C3)NC4=NC(CO4)(C)C)OC5=CC6=NC=NN6C=C5

PubChem CID

162623678

分子量

503.57

化学的性質と物理的性質

• 溶解度: DMSO : 125 mg/mL (248.23 mM; Need ultrasonic) H2O : <0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

よくある質問

What is the purity of this product?

This product is supplied at ≥99% 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 1429755-56-5, the molecular formula is C26H24N8O2.1/2C2H6O, and the molecular weight is 503.57 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.