PT2399|cas:1672662-14-4|西域试剂

PT2399,99.93%

产品编号：Bellancom-108697| CAS NO：1672662-14-4| 分子式：C₁₇H₁₀F₅NO₄S| 分子量：419.32

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货号	价格	库存与货期
Bellancom-108697	￥3700.00	杭州北京（现货）
Bellancom-108697	￥6200.00	杭州北京（现货）
Bellancom-108697	￥0.00	杭州北京（现货）
Bellancom-108697	￥0.00	杭州北京（现货）

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PT2399

产品介绍

PT2399 是一种高效、选择性的 HIF-2α 的拮抗剂，能直接结合 HIF-2α PAS B 结构域，IC₅₀ 值为 6 nM。PT2399 具有高效的体内抗肿瘤活性。

生物活性

PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC₅₀ of 6 nM. PT2399 displays potent antitumor activity in vivo.

体外研究

PT2399 (compound 10f) inhibits HIF-2α with an IC₅₀ of 6 nM.
PT2399 can bind directly to the HIF-2α PAS B domain, and cripple HIF-2α’s ability to bind to Aryl hydrocarbon receptor nuclear translocator (ARNT).
PT2399 (20 μM) causes off-target toxicity because it inhibits the proliferation of HIF-2α −/− 786-O cells and other cancer cell lines with undetectable HIF-2α.
PT2399 (0.2–2 μM; 0-21 days) inhibits 786-O cells soft agar growth.
PT2399 represses various HIF target genes in 786-O VHL−/− ccRCC cells, does not suppress HIF-1α-specific targets such as BNIP3.

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

Cell Viability Assay

Cell Line:	786-O cells
Concentration:	0 μM, 0.2 μM, 2 μM
Incubation Time:	0-21 days
Result:	Inhibited 786-O cell soft agar growth at 0.2–2 μM.

体内研究
(In Vivo)

PT2399 inhibits tumor cell proliferation 3.5 fold in renal cell carcinoma (RCC) bearing mice.
PT2399 reduces tumor cell density and increases fibrosis in RCC bearing mice.
PT2399 (100 mg/kg; oral gavage; every 12 hours) is more active than SU 11248, and inhibits tumor growth in several SU 11248-resistant tumors in RCC bearing mice .
PT2399 directly inhibits HIF-2α causes tumor regression in preclinical models of primary and metastatic pVHL-defective ccRCC in an on-target fashion.

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

Animal Model:	Mice with RCC tumorgraft
Dosage:	100 mg/kg
Administration:	Oral gavage; every 12 hours
Result:	More active than SU 11248, and inhibited tumor growth in several SU 11248-resistant tumors.

体内研究

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

Animal Model:	Mice with RCC tumorgraft
Dosage:	100 mg/kg
Administration:	Oral gavage; every 12 hours
Result:	More active than SU 11248, and inhibited tumor growth in several SU 11248-resistant tumors.

体内研究

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

Animal Model:	Mice with RCC tumorgraft
Dosage:	100 mg/kg
Administration:	Oral gavage; every 12 hours
Result:	More active than SU 11248, and inhibited tumor growth in several SU 11248-resistant tumors.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 200 mg/mL (476.96 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	2.3848 mL	11.9241 mL	23.8481 mL
5 mM	0.4770 mL	2.3848 mL	4.7696 mL
10 mM	0.2385 mL	1.1924 mL	2.3848 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 (stored under nitrogen)。-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: ≥ 1.67 mg/mL (3.98 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (3.98 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 16.7 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: ≥ 1.67 mg/mL (3.98 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (3.98 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 16.7 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: ≥ 1.67 mg/mL (3.98 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (3.98 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 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。