CP-31398 dihydrochloride

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CP-31398 dihydrochloride  纯度: 99.16%

CP-31398 dihydrochloride 在 p53 突变或野生型的癌细胞中，稳定 p53 的活性构象、促进 p53 的活性。

CP-31398 dihydrochloride

CP-31398 dihydrochloride Chemical Structure

CAS No. : 1217195-61-3

规格 价格 是否有货 数量
5 mg ￥800 In-stock
10 mg ￥1300 In-stock
25 mg ￥2500 In-stock
50 mg ￥4000 In-stock
100 mg ￥6500 In-stock
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生物活性

CP-31398 dihydrochloride stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53[1][2][3].

体外研究
(In Vitro)

CP-31398 (36.75 μM, 16 h) induces p21 in p53-mutant cells[1].
CP-31398 (15 μg/mL, 20 hours) could induce apoptosis and cell cycle arrest in SW480 cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Saos-2 cells expressing transfected mutant p53.
Concentration: 36.75 μM.
Incubation Time: 16 h.
Result: Induction of p21 in cells expressing only mutant p53.

Western Blot Analysis[3]

Cell Line: LN-18 and U87MG cells.
Concentration: 36 μM.
Incubation Time: 16 h.
Result: Decreased the levels of procaspase 3 and induced cleavage of caspase 7.

体内研究
(In Vivo)

CP-31398 (100 mg/kg, orally) exhibits significant anti-tumor activity in mice models[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Small human tumor xenografts in mice[1].
Dosage: 100 mg/kg.
Administration: Orally twice daily for 7 days.
Result: Suppressed A375.S2 tumor growth by -50%.

分子量

435.39

Formula

C22H28Cl2N4O
CAS 号

1217195-61-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro: 

DMSO : 8.33 mg/mL (19.13 mM; ultrasonic and warming and heat to 65°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2968 mL 11.4840 mL 22.9679 mL
5 mM 0.4594 mL 2.2968 mL 4.5936 mL
10 mM 0.2297 mL 1.1484 mL 2.2968 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: 0.83 mg/mL (1.91 mM); Suspended solution; Need ultrasonic

    此方案可获得 0.83 mg/mL (1.91 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 8.3 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: 0.83 mg/mL (1.91 mM); Suspended solution; Need ultrasonic

    此方案可获得 0.83 mg/mL (1.91 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 8.3 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
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. B A Foster, et al. Pharmacological rescue of mutant p53 conformation and function. Science. 1999 Dec 24;286(5449):2507-10.

    [2]. Rishu Takimoto, et al. The Mutant p53-Conformation Modifying Drug, CP-31398, Can Induce Apoptosis of Human Cancer Cells and Can Stabilize Wild-Type p53 Protein. Cancer Biol Ther. Jan-Feb 2002;1(1):47-55.

    [3]. J Wischhusen, et al. CP-31398, a novel p53-stabilizing agent, induces p53-dependent and p53-independent glioma cell death. Oncogene. 2003 Nov 13;22(51):8233-45.

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