ODM-203|cas:1430723-35-5|西域试剂

ODM-203,99.91%

产品编号：Bellancom-119367| CAS NO：1430723-35-5| 分子式：C₂₆H₂₁F₂N₅O₂S| 分子量：505.54

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-119367	￥600.00	杭州北京（现货）
Bellancom-119367	￥1250.00	杭州北京（现货）
Bellancom-119367	￥1950.00	杭州北京（现货）
Bellancom-119367	￥3900.00	杭州北京（现货）
Bellancom-119367	￥6400.00	杭州北京（现货）

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ODM-203

产品介绍

ODM-203 是一种口服有效的，具有选择性的 FGFR/VEGFR 抑制剂，其对 FGFR3/1/2 和 VEGFR3/2/1/4 的 IC₅₀ 值分别为 6, 11, 16, 5, 9, 26 和 35 nM。ODM-203 具有很强的抗肿瘤活性，并能激活肿瘤微环境中的免疫反应。

生物活性

ODM-203 is an orally active and selective FGFR/VEGFR inhibitor with IC₅₀ values of 6, 11, 16, 5, 9, 26 and 35 nM for FGFR3/1/2 and VEGFR3/2/1/4, respectively. ODM-203 has strong anti-tumour activity and activates immune responses in the tumour microenvironment.

体外研究

ODM-203 (eight-dose concentration series up to 3 μM; 96 h) potently inhibits FGFR signaling and proliferation in several FGFR-dependent cell lines.
ODM-203 (eight-dose concentration series up to 3 μM; 10 days) inhibits endothelial tubule formation.
ODM-203 (1, 10, 100, 1000 nM; 1 h) inhibiting FGFR and VEGFR cellular signaling in HUVEC cells.

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

Cell Viability Assay

Cell Line:	H1581 (ATCC-CRL-5878), SNU16 (ATCC-CRL-5974) and RT4 (HTB2) cells
Concentration:	Eight-dose concentration series up to 3 μM
Incubation Time:	96 h
Result:	Suppressed cell proliferation in a dose-dependent manner in H1581 (IC₅₀=104 nM), SNU16 (IC₅₀=132 nM) and RT4 cells (IC₅₀=192 nM).

Cell Viability Assay

Cell Line:	HUVECs and human umbilical vein endothelial cells (co-culture)
Concentration:	Eight-dose concentration series up to 3 μM
Incubation Time:	10 days (media and test agents were replaced every 2-3 days)
Result:	Inhibited endothelial tubule formation in a dose-dependent manner at non-toxic concentrations with an IC₅₀ value of 33 nM.

Western Blot Analysis

Cell Line:	HUVEC cells
Concentration:	1, 10, 100, 1000 nM
Incubation Time:	1 h
Result:	Suppressed both FGFR and VEGFR signaling.

体内研究
(In Vivo)

ODM-203 (20, 40 mg/kg; p.o.; single daily for 21 days) inhibits FGFR phosphorylation and tumor growth in several FGFR-dependent xenografts by suppressing FGFR signaling in tumors.
ODM-203 (7, 20, 40 mg/kg; p.o.; single daily for 21 days) shows strong anti-tumor activity in a VEGFR-dependent angiogenic orthotopic syngenic model (Renca) and suppresses angiogenesis.
ODM-203 (20, 40 mg/kg; p.o.; single daily for 5 days) activates immune response in the tumor microenvironment.

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

Animal Model:	Athymic Nude-Foxn1nu female mice (9-week-old; subcutaneous xenograft models).
Dosage:	20, 40 mg/kg
Administration:	Oral administration; single daily for 21 days.
Result:	Significantly inhibited tumour growth for 21 consecutive days. Showed tumor growth inhibition (TGI) in RT4 xenografts was 37% and 92% with dosage of 20 and 40 mg/kg, respectively.

Animal Model:	Male balb/c mice (8-week-old; orthotopic renca syngenic model).
Dosage:	7, 20, 40 mg/kg
Administration:	Oral administration; single daily for 21 days.
Result:	Showed tumor growth inhibition were 39%, 58% and 75% for dosage of 7, 20 and 40 mg/kg, respectively. Inhibited formation of lung metastasis, and suppressed angiogenesis.

Animal Model:	Male balb/c male mice (5 to 7-week-old; renca subcutaneous tumor model).
Dosage:	20, 40 mg/kg
Administration:	Oral administration; single daily for 5 days.
Result:	Resulted in an increase in the percentage of total and CD4 T cells. Decreased the expression of immune check points PD-1 and PD-L1 and increased IFN-γ expression on both CD8 T cells and NK cells.

体内研究

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

Animal Model:	Athymic Nude-Foxn1nu female mice (9-week-old; subcutaneous xenograft models).
Dosage:	20, 40 mg/kg
Administration:	Oral administration; single daily for 21 days.
Result:	Significantly inhibited tumour growth for 21 consecutive days. Showed tumor growth inhibition (TGI) in RT4 xenografts was 37% and 92% with dosage of 20 and 40 mg/kg, respectively.

Animal Model:	Male balb/c mice (8-week-old; orthotopic renca syngenic model).
Dosage:	7, 20, 40 mg/kg
Administration:	Oral administration; single daily for 21 days.
Result:	Showed tumor growth inhibition were 39%, 58% and 75% for dosage of 7, 20 and 40 mg/kg, respectively. Inhibited formation of lung metastasis, and suppressed angiogenesis.

Animal Model:	Male balb/c male mice (5 to 7-week-old; renca subcutaneous tumor model).
Dosage:	20, 40 mg/kg
Administration:	Oral administration; single daily for 5 days.
Result:	Resulted in an increase in the percentage of total and CD4 T cells. Decreased the expression of immune check points PD-1 and PD-L1 and increased IFN-γ expression on both CD8 T cells and NK cells.

体内研究

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

Animal Model:	Athymic Nude-Foxn1nu female mice (9-week-old; subcutaneous xenograft models).
Dosage:	20, 40 mg/kg
Administration:	Oral administration; single daily for 21 days.
Result:	Significantly inhibited tumour growth for 21 consecutive days. Showed tumor growth inhibition (TGI) in RT4 xenografts was 37% and 92% with dosage of 20 and 40 mg/kg, respectively.

Animal Model:	Male balb/c mice (8-week-old; orthotopic renca syngenic model).
Dosage:	7, 20, 40 mg/kg
Administration:	Oral administration; single daily for 21 days.
Result:	Showed tumor growth inhibition were 39%, 58% and 75% for dosage of 7, 20 and 40 mg/kg, respectively. Inhibited formation of lung metastasis, and suppressed angiogenesis.

Animal Model:	Male balb/c male mice (5 to 7-week-old; renca subcutaneous tumor model).
Dosage:	20, 40 mg/kg
Administration:	Oral administration; single daily for 5 days.
Result:	Resulted in an increase in the percentage of total and CD4 T cells. Decreased the expression of immune check points PD-1 and PD-L1 and increased IFN-γ expression on both CD8 T cells and NK cells.

性状

Solid

溶解性数据

In Vitro:

DMSO : 66.67 mg/mL (131.88 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9781 mL	9.8904 mL	19.7808 mL
5 mM	0.3956 mL	1.9781 mL	3.9562 mL
10 mM	0.1978 mL	0.9890 mL	1.9781 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 (4.11 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.11 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。
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 (4.11 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.11 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.11 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.11 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。