Vamotinib PF-114|cas:1416241-23-0|西域试剂

Vamotinib PF-114,98.69%

产品编号：Bellancom-147414| CAS NO：1416241-23-0| 分子式：C₂₉H₂₇F₃N₆O| 分子量：532.56

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-147414	￥4000.00	杭州北京（现货）
Bellancom-147414	￥6500.00	杭州北京（现货）
Bellancom-147414	￥13000.00	杭州北京（现货）

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Vamotinib PF-114

产品介绍

Vamotinib (PF-114) 是一种有效的，选择性具有口服活性的酪氨酸激酶抑制剂。Vamotinib 抑制 BCR/ABL 和 BCR/ABL-T315I 的自磷酸化。Vamotinib 诱导细胞凋亡 (apoptosis)。Vamotinib 显示出抗增殖和抗肿瘤活性。Vamotinib 在耐药性费城染色体阳性 (Ph+) 白血病的研究中具有潜力。

生物活性

Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia.

体外研究

Vamotinib (0-1 µM) inhibits ABL kinase and its mutants with IC₅₀s of 0.49, 0.78, 1.0 µM for ABL, ABL(T315l), ABL(H396P), respectively.
Vamotinib (0-1000 nM) inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I in a dose-dependent manner.
Vamotinib (0-2000 nM) shows anti-proliferative activity in Ba/F3 cells expressing native BCR/ABL.
Vamotinib (0-100 nM) induces apoptosis in Ba/F3 cells expressing BCR/ABL and BCR/ABL-T315I.
Vamotinib (0-1000 nM) inhibits the growth of Ph+ patient-derived cell lines in k562, kcl-22, SupB15, Tom-1, BV-173 cells.
Vamotinib (0-1000 nM) suppresses growth of Ph+ PD-LTC with nonmutational resistance as well as T315I mutation.

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

Western Blot Analysis

Cell Line:	Ba/F3 cells
Concentration:	0, 10, 25, 50, 100, 500, 1000 nM
Incubation Time:
Result:	Inhibited the autophosphorylation of BCR/ABL and BCR/ABL-T315I in a dose-dependent manner and inhibited substrate phosphorylation as shown by the reduced Crkl-phosphorylation and downstream activation of Stat5 by BCR/ABL, as well as by BCR/ABL-T315I.

Cell Proliferation Assay

Cell Line:	Ba/F3 cells
Concentration:	0, 50, 500, 2000 nM
Incubation Time:
Result:	Potently inhibited proliferation of Ba/F3 cells expressing native BCR/ABL in a dose-dependent manner and shows no effects on empty vector-transduced Ba/F3 cells in the presence of IL-3 (10 ng/ml).

Apoptosis Analysis

Cell Line:	Ba/F3 cells
Concentration:	0-100 nM
Incubation Time:
Result:	Induced apoptosis in Ba/F3 cells expressing BCR/ABL and BCR/ABL-T315I in a dose dependent manner.

体内研究
(In Vivo)

Vamotinib (25, 40 mg/kg; i.g.; daily for 14 consecutive days) shows anti-tumor activity.
Vamotinib (50 mg/kg; p.o.; once daily for 20 days) prolongs the survival of mice with both BCR/ABL- and BCR/ABL-T315I-driven CML-like disease.

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

Animal Model:	Female BALB/cAnNRj-Foxn1nu mice (K562 nude mouse xenograft model)
Dosage:	25, 40 mg/kg
Administration:	Oral gavage; daily for 14 consecutive days
Result:	Caused a 100% reduction of the mean tumor volume within 4 weeks.

Animal Model:	8-12 weeks, C57BL/6N mice (CML-like disease mouse model)
Dosage:	50 mg/kg
Administration:	P.o.; once daily for 20 days
Result:	Extended median survival significantly from 28 days to 39.

体内研究

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

Animal Model:	Female BALB/cAnNRj-Foxn1nu mice (K562 nude mouse xenograft model)
Dosage:	25, 40 mg/kg
Administration:	Oral gavage; daily for 14 consecutive days
Result:	Caused a 100% reduction of the mean tumor volume within 4 weeks.

Animal Model:	8-12 weeks, C57BL/6N mice (CML-like disease mouse model)
Dosage:	50 mg/kg
Administration:	P.o.; once daily for 20 days
Result:	Extended median survival significantly from 28 days to 39.

体内研究

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

Animal Model:	Female BALB/cAnNRj-Foxn1nu mice (K562 nude mouse xenograft model)
Dosage:	25, 40 mg/kg
Administration:	Oral gavage; daily for 14 consecutive days
Result:	Caused a 100% reduction of the mean tumor volume within 4 weeks.

Animal Model:	8-12 weeks, C57BL/6N mice (CML-like disease mouse model)
Dosage:	50 mg/kg
Administration:	P.o.; once daily for 20 days
Result:	Extended median survival significantly from 28 days to 39.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (93.89 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8777 mL	9.3886 mL	18.7772 mL
5 mM	0.3755 mL	1.8777 mL	3.7554 mL
10 mM	0.1878 mL	0.9389 mL	1.8777 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 and light)。-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: 2.5 mg/mL (4.69 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (4.69 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (4.69 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.69 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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