RP-1664 - CAS:2980682-00-4

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RP-1664

目录号 : KM32561 CAS No. : 2980682-00-4 纯度 : 98%

Data Sheet 产品使用指南

RP-1664 是一种具有选择性并且口服有效的 PLK4 抑制剂，其 IC50 值为 3 nM。RP-1664 对相关激酶 (包括 AURKA/B 和 PLK1) 表现出高度选择性。RP-1664 能破坏癌细胞中心粒的生物合成，并且导致 PLK4 和 p21 蛋白的积累。RP-1664 对 TRIM37 高表达的细胞或者肿瘤更敏感。RP-1664 在乳腺癌和神经母细胞瘤研究中显示出抗肿瘤活性。

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
1mg		In-stock
5mg		In-stock

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生物活性

RP-1664 is a selective and orally active PLK4 inhibitor with an IC50 of 3 nM. RP-1664 demonstrates exquisite selectivity over related kinases, including AURKA/B and PLK1. RP-1664 disrupts centriole biogenesis in cancer cells and leads an accumulation of PLK4 and p21 protein. RP-1664 demonstrates increased sensitivity in TRIM37-high-expressing cells or tumors. RP-1664 exhibits anti-tumor activity in breast cancer and neuroblastoma research[1][2].

IC₅₀&Target

PLK4

体外研究

RP-1664 (1-1000 nM, 48-72 h) dose-dependently upregulates the total PLK4 protein levels in RPE1-hTERT Cas9 TP53 knockout cells and increases p21 protein expression in RPE1-hTERT Cas9 TP53 wild-type cells [1].
RP-1664 (0.001-10 μM) demonstrated approximately 30-fold increased sensitivity in TRIM37-overexpressing/TP53 wild-type cells compared to TRIM37-normal/TP53-knockout cells, while showing moderate activity in TRIM37-high-expressing/TP53-knockout cells and TRIM37-normal/TP53-wild-type cells [1].
RP-1664 (1-1000 nM, 48-72 h) induces centrosome loss in p53 wild-type and p53-deficient RPE1 cells, as well as three distinct neuroblastoma cell lines (CHP134, CHP212, SHSY5Y), at concentrations > 100 nM [1].
RP-1664 (1-1000 nM, 48-72 h) can induce supernumerary centrosomes in RPE1 cells with normal and p53-deficient conditions within the concentration range of 25-100 nM [1].
RP-1664 (0-2000 nM, 48 h) enhances cellular sensitivity to PLK4 inhibition and centrosome depletion in a manner dependent on high TRIM37 protein levels and functional p53 [1].
The EC50 of RP-1664 (compound 37) in reducing the viability of MCF7 cells was 0.051 μM [2].

Western Blot Analysis

Cell Line:	RPE1-hTERT Cas9 TP53-null cells and RPE1-hTERT Cas9 TP53-WT cells
Concentration:	1-1000 nM
Incubation Time:	48-72 h
Result:	Increased total PLK4 protein levels in RPE1-hTERT Cas9 TP53-null cells. Increased p21 protein levels in RPE1-hTERT Cas9 TP53-WT cells dose dependently.

体内研究

RP-1664 (600 ppm, administered orally via feed, with dosing schedules of 7 days on/7 days off, 14 days on/7 days off, or daily dosing for 40 days) demonstrated dose-dependent antitumor activity in the MCF7 xenograft mouse model [1].
RP-1664 (300 ppm, administered orally via feed, dosing for 17 days followed by a 7-day break, repeated for 40 days) demonstrated significant antitumor effects in the NBL model through a low-dose-induced centrosome amplification mechanism [1].
RP-1664 (compound 37) (6-21 mg/kg, oral administration, twice daily for 35 days) demonstrated dose-dependent tumor growth inhibition effects, including growth arrest and tumor regression, in the CAL-148 xenograft mouse model [2].
RP-1664 (300-600 ppm, administered orally via feed, dosing schedules of 3 days on/4 days off, 14 days on/7 days off, or daily dosing for 55 days) effectively inhibits tumor growth in CHP-134 xenograft mice [2].

Animal Model:	Female BALB/c Nude mice were supplemented with estradiol in drinking water (2.5 µg/mL) and gamma irradiated (1.2 Gy) 1 week and 24-72 hours prior to inoculation in the right flank using 10 million MCF7 cells
Dosage:	600 ppm
Administration:	p.o. on schedules of 7 days on/7 off or 14 days on/7 off or daily for 40 days
Result:	Inhibited the tumor growth with maximal tumor growth inhibition (TGI) of 95% at 600 parts per million (ppm).

Animal Model:	Female CB/17 SCID mice were inoculated in the right flank with 10 million cells of either parental CHP134, CHP134 TP53-KO or CHP134 TRIM37-KO
Dosage:	300 ppm
Administration:	p.o. on schedules of 17 days on/7 off for 40 days
Result:	Suppressed tumor growth regardless of TRIM37 or TP53 inactivation.

Animal Model:

Female SCID-beige mice xenografted with CAL-148 cells (5-7 weeks) (10⁷ cells per mouse)

Dosage:

6, 11, 21 mg/kg

Administration:

i.g. for 35 days

Result:

Showed tumor growth inhibition at 6 mg/kg.
Showed tumor growth stasis at 11 mg/kg.
Showed tumor growth regressions at 21 mg/kg.
Increased protein levels of PLK4 or p21 for 4 to 11 days.

Animal Model:	Female CB-17 SCID mice bearing subcutaneous CHP-134 xenografts (5-7 weeks) (10⁷ cells per mouse)
Dosage:	300, 600 ppm
Administration:	p.o. on schedules of 3 days on/4 off or 14 days on/7 off or daily for 55 days
Result:	Improved the tumor regressions efficacy with longer continuous exposure. Improved tolerability with intermittent dosing, whereas continuous dosing at 600 ppm was not tolerated beyond day 46. Increased protein levels of PLK4 or p21 for 4 to 11 days.

分子式

C₂₃H₂₄F₂N₈O₂S

分子量

514.55

CAS号

2980682-00-4

中文名称

5-环丙基-2-N-(2,6-二氟-4-甲磺酰基苯基)-2-N-甲基-6-(1-甲基咪唑-4-基)-4-N-(5-甲基-1H-吡唑-3-基)嘧啶-2,4-二胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO: 100 mg/mL (194.34 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9434 mL	9.7172 mL	19.4345 mL
5 mM	0.3887 mL	1.9434 mL	3.8869 mL
10 mM	0.1943 mL	0.9717 mL	1.9434 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。

纯度： 98%

Data Sheet

产品使用指南

[1]. Isabel Soria-Bretones, et al. A dual mechanism of sensitivity to PLK4 inhibition by RP-1664 in neuroblastoma. bioRxiv. February 17, 2025.

[2]. Vallée F, et al. Discovery of RP-1664: A First-in-Class Orally Bioavailable, Selective PLK4 Inhibitor. J Med Chem. 2025 Jun 12;68(11):10631-10647.

The molarity calculator equation

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

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The dilution calculator equation

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

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动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

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工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器