2. Epigenetics
  3. Histone Methyltransferase
  4. MRTX-1719

MRTX-1719 是一种有效的，具有口服活性，选择性的 PRMT5•MTA 复合物抑制剂，对PRMT5•MTA 和 PRMT5 的 IC50 分别为 3.6 和 20.5 nM。MRTX-1719 可以与 PRMT5•MTA 复合物结合，KD 值为 0.14 pM。MRTX-1719 在体内外显示出抗肿瘤活性，可用于癌症研究。

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MRTX-1719 Chemical Structure

MRTX-1719 Chemical Structure

CAS No. : 2630904-45-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5165
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1 mg ￥2590
In-stock
5 mg ￥5050
In-stock
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Customer Review

Other Forms of MRTX-1719:

MRTX-1719 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MRTX-1719 is a potent, orally active, selective PRMT5•MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5•MTA and PRMT5. MRTX-1719 binds to the PRMT5•MTA complex, with KD value of 0.14 pM. MRTX-1719 shows antineoplastic activity in vitro and in vivo, and can be used for cancer study[1][2].

IC50 & Target[1]

PRMT5

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
> 10000 nM
Compound: (P)-27
Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
[PMID: 35041419]
HCT-116 IC50
12 nM
Compound: MRTX1719
Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as cell viability after 10 days by CellTiter-Glo assay
Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as cell viability after 10 days by CellTiter-Glo assay
[PMID: 35926325]
HCT-116 IC50
12 nM
Compound: (M)-27; MRTX1719
Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
[PMID: 35041419]
HCT-116 IC50
3470 nM
Compound: (P)-27
Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
[PMID: 35041419]
HCT-116 IC50
41 nM
Compound: 27
Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
[PMID: 35041419]
HCT-116 IC50
890 nM
Compound: MRTX1719
Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as cell viability after 10 days by CellTiter-Glo assay
Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as cell viability after 10 days by CellTiter-Glo assay
[PMID: 35926325]
HCT-116 IC50
890 nM
Compound: (M)-27; MRTX1719
Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
[PMID: 35041419]
HepG2 IC50
6600 nM
Compound: MRTX1719
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability measured after 120 hrs CellTiter-Glo assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability measured after 120 hrs CellTiter-Glo assay
[PMID: 35926325]
体外研究
(In Vitro)

MRTX-1719 (10 天) 在 MTAP 缺失的 HCT116 细胞而非野生型细胞中抑制 PRMT5 活性，IC50 为 8 nM[1]。
MRTX1719 (10 天) 在 MTAP 敲除的 HCT116 细胞中的 IC50 值为 12 nM，对野生型 HCT116 细胞的 IC50 值为 890 nM[1]。

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

MRTX-1719 相关抗体:
体内研究
(In Vivo)

MRTX1719 (12.5-100 mg/kg/每天，口服，21天) 可降低 Lu-99 原位异种移植肿瘤的生长[2]。

药代动力学分析[2]

Model Route Dose (mg/kg) Cltotal (mL/min/kg) Vdss (L/kg) t1/2 (h)
CD-1 mouse. i.v. 3 83 6.3 1.5
Beagle dog i.v. 2 14 3.4 4.8
Cynomolgus monkey i.v. 2 15 2.3 6.1
Model Route Dose (mg/kg) Cmax (ug/mL) AUCinf (h*ug/mL) F (%)
CD-1 mouse. p.o. 30 1.16 4.85 80
Beagle dog p.o. 10 1.40 7.47 59
Cynomolgus monkey p.o. 10 / / 41

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

Animal Model: Lu-99 (an MTAP/CDKN2A-deleted human lung cancer cell line ) xenograft tumor models[2]
Dosage: 12.5, 25, 50, and 100 mg/kg/d, 21 day
Administration: Oral gavage
Result: Reduced the tumor volume with 86% tumor growth inhibition (TGI) at 50 mg/kg and 88% TGI at 100 mg/kg.
Clinical Trial
分子量

464.88

Formula

C23H18ClFN6O2
CAS 号
性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (215.11 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1511 mL 10.7555 mL 21.5109 mL
5 mM 0.4302 mL 2.1511 mL 4.3022 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

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

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2 mg/mL (4.30 mM); 澄清溶液

    此方案可获得 ≥ 2 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2 mg/mL (4.30 mM); 悬浊液; 超声助溶

    此方案可获得 2 mg/mL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 20.0 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。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.40%

COA (181 KB) HNMR (292 KB) LCMS (95 KB)

产品使用指南 (1538 KB)
参考文献

MRTX-1719 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1511 mL 10.7555 mL 21.5109 mL 53.7773 mL
5 mM 0.4302 mL 2.1511 mL 4.3022 mL 10.7555 mL
10 mM 0.2151 mL 1.0755 mL 2.1511 mL 5.3777 mL
15 mM 0.1434 mL 0.7170 mL 1.4341 mL 3.5852 mL
20 mM 0.1076 mL 0.5378 mL 1.0755 mL 2.6889 mL
25 mM 0.0860 mL 0.4302 mL 0.8604 mL 2.1511 mL
30 mM 0.0717 mL 0.3585 mL 0.7170 mL 1.7926 mL
40 mM 0.0538 mL 0.2689 mL 0.5378 mL 1.3444 mL
50 mM 0.0430 mL 0.2151 mL 0.4302 mL 1.0755 mL
60 mM 0.0359 mL 0.1793 mL 0.3585 mL 0.8963 mL
80 mM 0.0269 mL 0.1344 mL 0.2689 mL 0.6722 mL
100 mM 0.0215 mL 0.1076 mL 0.2151 mL 0.5378 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MRTX-17192630904-45-7MRTX1719MRTX 1719Histone MethyltransferaseNSCLCCRCPRMT5MTAHCT116Lu-99Inhibitorinhibitorinhibit

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