Mobocertinib succinate 莫博替尼琥珀酸盐; TAK-788 succinate; AP32788 succinate|cas:2389149-74-8|西域试剂

Mobocertinib succinate 莫博替尼琥珀酸盐; TAK-788 succinate; AP32788 succinate,99.61%

产品编号：Bellancom-135815A| CAS NO：2389149-74-8| 分子式：C₃₆H₄₅N₇O₈| 分子量：703.78

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货号	价格	库存与货期
Bellancom-135815A	￥600.00	杭州北京（现货）
Bellancom-135815A	￥900.00	杭州北京（现货）
Bellancom-135815A	￥1500.00	杭州北京（现货）
Bellancom-135815A	￥2500.00	杭州北京（现货）
Bellancom-135815A	￥9500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Mobocertinib succinate 莫博替尼琥珀酸盐; TAK-788 succinate; AP32788 succinate

产品介绍

Mobocertinib (TAK-788) succinate 是一种口服有效并且不可逆的 EGFR/HER2 抑制剂。Mobocertinib succinate 能选择性地 (相较于野生型 EGFR) 抑制含有 EGFRex20ins 的致癌突变体。Mobocertinib succinate 可用于 NSCLC 的研究。

生物活性

Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research.

体外研究

Mobocertinib succinate (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC₅₀ of 21 nM.
Mobocertinib succinate (2 h) potently inhibits EGFR with common activating mutations (HCC827 (D), HCC4011 (L)) or with a T790M mutation (H1975 (LT)) more potently than WT EGFR (A431 (WT)).
Mobocertinib succinate (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells.
Mobocertinib succinate (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling.
Mobocertinib succinate (0.01, 0.1 and 1 μM; 6 h) inhibits HER2 signaling in H1781 (HER2 Exon 20^G776>VC), Ba/F3 (HER2 exon 20^YVMA) cells.

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

Cell Viability Assay

Cell Line:	LU0387 (NPH) cells
Concentration:	1.5 nM-10 μM
Incubation Time:	7 days
Result:	Showed good inhibition activity for LU0387 (NPH) cells with IC₅₀ of 21 nM.

Cell Viability Assay

Cell Line:	A431 (WT), HCC827 (D), HCC4011 (L), H1975 (LT) cells
Concentration:
Incubation Time:	2 h
Result:	Inhibited EGFR with common activating mutations of HCC827 (D), HCC4011 (L) cells and T790M mutation of H1975 (LT) with IC₅₀s of 4, 1.3 and 9.8 nM respectively, which more potently than WT EGFR (A431 (WT); IC₅₀ of 35 nM).

Western Blot Analysis

Cell Line:	CUTO14 (ASV) cells
Concentration:	0.1 nM-1 μM
Incubation Time:	6 h
Result:	Robustly inhibited EGFR signaling, reaching 80% and 100% inhibition of phosphorylated EGFR (pEGFR) at concentrations of 100 nM and 1 μM, respectively.

Western Blot Analysis

Cell Line:	HCC827 (D), HCC4011 (L), H1975 (LT) cells
Concentration:	0.3 nM-1 μM
Incubation Time:	6 h
Result:	Potently inhibited EGFR and downstream signaling in HCC827 (D), HCC4011 (L) and H1975 (LT) cells.

Western Blot Analysis

Cell Line:	H1781 (HER2 Exon 20^G776>VC), Ba/F3 (HER2 exon 20^YVMA) cells
Concentration:	0.01, 0.1 and 1 μM
Incubation Time:	6 h
Result:	Inhibited HER2 signaling in H1781 and Ba/F3-HER2 exon 20^YVMA mutant cells at 0.1 μM with significantly decreased phosphorylations of HER2, AKT, and ERK1/2 in a dose-dependent manner.

体内研究
(In Vivo)

Mobocertinib succinate (3, 10, 30 mg/kg; p.o.; once daily for 20 days) significantly induces tumor growth inhibition.

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

Animal Model:	Female Athymic Nude-Foxn1^nu mice (human NSCLC H1975 LT tumor model).
Dosage:	3, 10, 30 mg/kg
Administration:	Oral; once daily for 20 days.
Result:	Decreased the mean tumor volume by 44% and 92% when at 3 mg/kg and 10 mg/kg, respectively, relative to the tumor size of vehicle group. Induced a 76% tumor regression relative to the pretreatment tumor size at 30 mg/kg.

体内研究

Mobocertinib succinate (3, 10, 30 mg/kg; p.o.; once daily for 20 days) significantly induces tumor growth inhibition.

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

Animal Model:	Female Athymic Nude-Foxn1^nu mice (human NSCLC H1975 LT tumor model).
Dosage:	3, 10, 30 mg/kg
Administration:	Oral; once daily for 20 days.
Result:	Decreased the mean tumor volume by 44% and 92% when at 3 mg/kg and 10 mg/kg, respectively, relative to the tumor size of vehicle group. Induced a 76% tumor regression relative to the pretreatment tumor size at 30 mg/kg.

体内研究

Mobocertinib succinate (3, 10, 30 mg/kg; p.o.; once daily for 20 days) significantly induces tumor growth inhibition.

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

Animal Model:	Female Athymic Nude-Foxn1^nu mice (human NSCLC H1975 LT tumor model).
Dosage:	3, 10, 30 mg/kg
Administration:	Oral; once daily for 20 days.
Result:	Decreased the mean tumor volume by 44% and 92% when at 3 mg/kg and 10 mg/kg, respectively, relative to the tumor size of vehicle group. Induced a 76% tumor regression relative to the pretreatment tumor size at 30 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (177.61 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4209 mL	7.1045 mL	14.2090 mL
5 mM	0.2842 mL	1.4209 mL	2.8418 mL
10 mM	0.1421 mL	0.7104 mL	1.4209 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 (sealed storage, away from moisture)。-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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (2.96 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.96 mM，饱和度未知) 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (2.96 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.96 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。