Tucatinib hemiethanolate Irbinitinib hemiethanolate; ARRY-380 hemiethanolate; ONT-380 hemiethanolate|cas:1429755-56-5|西域试剂

Tucatinib hemiethanolate Irbinitinib hemiethanolate; ARRY-380 hemiethanolate; ONT-380 hemiethanolate,99.45%

产品编号：Bellancom-16069A| CAS NO：1429755-56-5| 分子式：C₂₆H₂₄N₈O₂.1/2C₂H₆O| 分子量：503.57

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货号	价格	库存与货期
Bellancom-16069A	￥500.00	杭州北京（现货）
Bellancom-16069A	￥900.00	杭州北京（现货）
Bellancom-16069A	￥1800.00	杭州北京（现货）
Bellancom-16069A	￥2500.00	杭州北京（现货）
Bellancom-16069A	￥4500.00	杭州北京（现货）

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Tucatinib hemiethanolate Irbinitinib hemiethanolate; ARRY-380 hemiethanolate; ONT-380 hemiethanolate

产品介绍

Tucatinib (Irbinitinib) hemiethanolate 是有效，具有口服活性的、选择性的 HER2抑制剂，IC₅₀ 为8 nM。

生物活性

Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC₅₀ of 8 nM.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 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.

体内研究

西域 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (248.23 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9858 mL	9.9291 mL	19.8582 mL
5 mM	0.3972 mL	1.9858 mL	3.9716 mL
10 mM	0.1986 mL	0.9929 mL	1.9858 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.08 mg/mL (4.13 mM); Clear solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.13 mM) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (4.13 mM); Clear solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.13 mM) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.13 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.13 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。