Alofanib - CAS:1612888-66-0

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Alofanib (Synonyms:RPT835)

目录号 : KM14300 CAS No. : 1612888-66-0 纯度 : 98%

Data Sheet 产品使用指南

Alofanib (RPT835)是高效和选择性的成纤维细胞生长因子受体2 (FGFR2) 的变构抑制剂。抗癌活性。抗血管生成活性。

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10mg		In-stock
25mg		In-stock
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100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer and antiangiogenic activity.

体外研究

Alofanib inhibits phosphorylation of FRS2α with IC₅₀s of 7 and 9 nM in hFOB and SUM 52PE cells expressing different FGFR2 isoforms.

Alofanib (0.2-0.8 μM, 6 hours) inhibits FGF-mediated proliferation in a panel of four cell lines representing several tumour types (triple-negative breast cancer, melanoma, and ovarian cancer) with GI₅₀s of 16-370 nM.

Cell Proliferation Assay

Cell Line:	SKOV3, HS478T, Mel Kor cells
Concentration:	0.2, 0.4, 0.8 μM
Incubation Time:	6 hours after dosing, FGF2 is added at a concentration of 25 ng/ml
Result:	Inhibited growth of SKOV3 and HS578T cells with GI₅₀s of 0.37 and 0.21 μM. Did not potently inhibit growth of Mel Kor cells that do not contain FGFR2 (GI₅₀>10 μM).

体内研究

In a FGFR-driven human tumour xenograft model, oral administration of alofanib (30 mg/kg, gavage, daily, 40 days, N=10) is well tolerated and results in potent antitumour activity.

Treatment with alofanib (10 mg/kg/d, 0, 3 and 6 d, intraperitoneally) ablates experimental FGF-induced angiogenesis in vivo.

Animal Model:	C57Bl/6 × DBA/2 F1 mice of 22–30 g
Dosage:	10 mg/kg/d
Administration:	Intraperitoneally, 0, 3 and 6 d
Result:	Alofanib inhibits angiogenesis in mouse models.

分子式

C₁₉H₁₅N₃O₆S

分子量

413.40

CAS号

1612888-66-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 30.1 mg/mL (72.81 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4190 mL	12.0948 mL	24.1896 mL
5 mM	0.4838 mL	2.4190 mL	4.8379 mL
10 mM	0.2419 mL	1.2095 mL	2.4190 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 (5.03 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.03 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 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。

临床试验

科研文献

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

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KKL 顾客使用本产品发表的 3 篇科研文献

The molarity calculator equation

The dilution calculator equation