RPI-1|cas:269730-03-2|西域试剂

RPI-1,98.97%

产品编号：Bellancom-101246| CAS NO：269730-03-2| 分子式：C₁₇H₁₅NO₄| 分子量：297.31

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货号	价格	库存与货期
Bellancom-101246	￥600.00	杭州北京（现货）
Bellancom-101246	￥1000.00	杭州北京（现货）
Bellancom-101246	￥2000.00	杭州北京（现货）
Bellancom-101246	￥3000.00	杭州北京（现货）
Bellancom-101246	￥4500.00	杭州北京（现货）

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RPI-1

产品介绍

RPI-1 是一种特异的口服 2-吲哚啉酮 Ret 酪氨酸激酶抑制剂。RPI-1 抑制人甲状腺髓样癌 TT 细胞增殖、Ret 酪氨酸磷酸化、Ret 蛋白表达及 PLCgamma、ERKs 和 AKT 的活化。具有抗肿瘤活性。

生物活性

RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity.

体外研究

TPC-1 cells are sensitive to the growth inhibitory effect of RPI-1 with an IC₅₀ of 5.1 μM, following 72 hours of treatment. RPI-1 (7.5-60 µM) inhibits Ret/Ptc1 autophosphorylation in TPC-1 cells. RPI-1 inhibitory effects in the TPC-1 cell culture conditions lead to inhibition of pathways involving JNK2 and AKT.
The RPI-1 IC₅₀ value for cell proliferation is 3.6 µM in NIH3T3 cells expressing the Ret mutant compared with 16 µM in non-transfected NIH3T3 cells, and that for colony formation in soft agar was 2.4 µM and 26 µM in RET mutant-transfected and H-RAS-transfected NIH3T3 cells, respectively. In NIH3T3 cells expressing the Ret mutant, Ret protein and tyrosine phosphorylation were undetectable after 24 hours of RPI-1 treatment. In TT cells, RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT.

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

体内研究

RPI-1 (50, 100 mg/kg; p.o.; twice a day for 10 days) inhibits the tumor growth of TT xenografts by 81%.

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

Animal Model:	8- to 11-week-old female athymic nude CD-1 mice (bearing TT cells)
Dosage:	50, 100 mg/kg
Administration:	P.o.; twice a day for 10 days
Result:	A dose-dependent effect on tumor growth was observed, with a dose of 250 mg/kg/day resulting in less tumor weight inhibition than the 2100mg/kg/day dose after 10 days of treatment.

体内研究

RPI-1 (50, 100 mg/kg; p.o.; twice a day for 10 days) inhibits the tumor growth of TT xenografts by 81%.

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

Animal Model:	8- to 11-week-old female athymic nude CD-1 mice (bearing TT cells)
Dosage:	50, 100 mg/kg
Administration:	P.o.; twice a day for 10 days
Result:	A dose-dependent effect on tumor growth was observed, with a dose of 250 mg/kg/day resulting in less tumor weight inhibition than the 2100mg/kg/day dose after 10 days of treatment.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (420.44 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3635 mL	16.8175 mL	33.6349 mL
5 mM	0.6727 mL	3.3635 mL	6.7270 mL
10 mM	0.3363 mL	1.6817 mL	3.3635 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 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (7.00 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (7.00 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 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