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蛋白质酪氨酸激酶
/ FLT3 / MRX-2843

MRX-2843 {[allProObj[0].p_purity_real_show]}

货号：A188034 同义名： UNC2371

MRX-2843（UNC2371）是一种口服活性、ATP竞争性的MERTK和FLT3酪氨酸激酶抑制剂（TKI），其IC50值分别为1.3 nM和0.64 nM。

MRX-2843 化学结构 CAS号：1429882-07-4
MRX-2843 化学结构
CAS号：1429882-07-4
MRX-2843 3D分子结构
CAS号：1429882-07-4
MRX-2843 化学结构 CAS号：1429882-07-4
MRX-2843 3D分子结构 CAS号：1429882-07-4
规格 价格 会员价 库存 数量
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MRX-2843 纯度/质量文件 产品仅供科研

货号：A188034 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 FLT3 ↓ 其他靶点 纯度
R406 ✔ Syk 98%
Go6976 ✔ 99%+
Quizartinib +++

FLT3 (ITD), IC50: 1.1 nM

FLT3 (WT), IC50: 4.2 nM

 		98%
Gilteritinib ++++

FLT3, IC50: 0.29 nM

 		99%+
Amuvatinib +

FLT3 (D835Y), IC50: 81 nM

 		99%+
Pacritinib ++

FLT3, IC50: 22 nM

FLT3 (D835Y), IC50: 6 nM

 		97%
Dovitinib ++++

FLT3, IC50: 1 nM

 		c-Kit 99%+
Denfivontinib ++++

FLT3 (D835Y), IC50: 0.4 nM

FLT3, IC50: 0.4 nM

 		RET 99%+
TAK-659 HCl ++

FLT3, IC50: 4.6 nM

 		Syk 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

MRX-2843 细胞实验

Cell Line
Concentration Treated Time Description References
GL261 88.6 nM MRX-2843 inhibits cell growth Neurooncol Adv. 2020 Jun 3;2(1):vdaa065
GSC407 217.7 nM 48 hours MRX-2843 inhibits cell growth and induces apoptosis Neurooncol Adv. 2020 Jun 3;2(1):vdaa065
GSC923 288.1 nM 48 hours MRX-2843 inhibits cell growth and induces apoptosis Neurooncol Adv. 2020 Jun 3;2(1):vdaa065
H1650 300 nM 3-4 days Evaluate the effect of MRX-2843 on EGFR-mutant NSCLC cells J Clin Invest. 2022 Aug 1;132(15):e150517
H4006 300 nM 3-4 days Evaluate the effect of MRX-2843 on EGFR-mutant NSCLC cells J Clin Invest. 2022 Aug 1;132(15):e150517
NOMO-1 150-300 nM 72 hours MRX-2843 induced apoptosis and inhibited colony formation. JCI Insight. 2016 Mar;1(3):e85630
Kasumi-1 10-300 nM 1 hour MRX-2843 inhibited MERTK phosphorylation and downstream signaling pathways ERK1/2, AKT, and STAT6, leading to apoptosis and reduced colony formation. JCI Insight. 2016 Mar;1(3):e85630
U251 95.5 nM 48 hours MRX-2843 inhibits cell growth and induces apoptosis Neurooncol Adv. 2020 Jun 3;2(1):vdaa065
MV4-11 50-100 nM 72 hours MRX-2843 induced apoptosis and inhibited colony formation. JCI Insight. 2016 Mar;1(3):e85630
Jurkat cells 300 nM 48 hours MRX-2843 induced cell death Cancers (Basel). 2022 Dec 13;14(24):6142
PEER cells 10-100 nM 1 hour MRX-2843 inhibited MERTK activation with IC50 of 3.9 nM Cancers (Basel). 2022 Dec 13;14(24):6142
Loucy cells 10-100 nM 1 hour MRX-2843 inhibited MERTK activation with IC50 of 9.5 nM Cancers (Basel). 2022 Dec 13;14(24):6142
MOLM-14 50 nM 48 hours MRX-2843 inhibited FLT3-ITD activation and downstream signaling pathways, leading to apoptosis and reduced colony formation. JCI Insight. 2016 Mar;1(3):e85630
HMC-3 100 nM MRX-2843 decreases cell viability Neurooncol Adv. 2020 Jun 3;2(1):vdaa065
Jurkat (T-ALL) 100 nM MRX-2843 and 1.4 nM vincristine 72 hours To evaluate the synergistic effect of MRX-2843 and vincristine, results showed that the combination significantly inhibited cell growth. J Control Release. 2023 Sep;361:470-482
TC32 cells 178-297 nM (IC50) 72 hours MRX-2843 resulted in a dose-dependent reduction in cell density with IC50 values ranging from 178 to 297 nM. Cancers (Basel). 2024 Aug 12;16(16):2831
RD-ES cells 178-297 nM (IC50) 72 hours MRX-2843 resulted in a dose-dependent reduction in cell density with IC50 values ranging from 178 to 297 nM. Cancers (Basel). 2024 Aug 12;16(16):2831
SK-ES-1 cells 178-297 nM (IC50) 72 hours MRX-2843 resulted in a dose-dependent reduction in cell density with IC50 values ranging from 178 to 297 nM. Cancers (Basel). 2024 Aug 12;16(16):2831
TC106 cells 34.5 nM (IC50) 1 hour MRX-2843 decreased phosphorylation of MERTK in a dose-dependent manner with an IC50 of 34.5 nM. Cancers (Basel). 2024 Aug 12;16(16):2831
A673 cells 13.3 nM (IC50) 1 hour MRX-2843 decreased phosphorylation of MERTK in a dose-dependent manner with an IC50 of 13.3 nM. Cancers (Basel). 2024 Aug 12;16(16):2831
697 B-ALL cells 5-25 nM to >250 nM Evaluate the inhibitory effect of MRX-2843 on MERTK phosphorylation JCI Insight. 2018 Nov 2;3(21):e97941
human alveolar bone mesenchymal stem cells 100 nM 21 days To evaluate the effect of MRX-2843 on osteogenic differentiation of alveolar bone MSCs. Results showed enhanced mineralization with MRX-2843 treatment. J Dent Res. 2023 Sep;102(10):1131-1140

MRX-2843 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude-Foxn1nu mice H4006 xenograft model Oral gavage 3 mg/kg OSI and 20 mg/kg MRX-2843 OSI once daily and MRX-2843 twice daily for 57 days Evaluate the effect of MRX-2843 in combination with OSI on tumor growth in EGFR-mutant NSCLC J Clin Invest. 2022 Aug 1;132(15):e150517
Nude mice A673 xenograft model Intraperitoneal injection 10 mg/kg Twice a week for 28 days MRX-2843 enhances irinotecan-mediated tumor growth suppression effects in Ewing sarcoma murine models Nat Commun. 2024 Jun 21;15(1):5292
Mice Xenograft model Oral 50-75 mg/kg Once daily until study end MRX-2843 significantly prolonged survival in xenograft models of FLT3-ITD or MERTK-positive AML. JCI Insight. 2016 Mar;1(3):e85630
NSG mice Jurkat T-ALL cell line xenograft model Oral 75 mg/kg Once daily for 28 days MRX-2843 significantly reduced disease burden and prolonged survival Cancers (Basel). 2022 Dec 13;14(24):6142
Mice GL261 syngeneic orthotopic glioblastoma model Oral gavage 50 mg/kg Daily for 14 days MRX-2843 extends survival and reduces immunosuppression and angiogenesis in the tumor microenvironment Neurooncol Adv. 2020 Jun 3;2(1):vdaa065
Mice 697 B-ALL xenograft model Oral 3, 25, or 75 mg/kg single oral dose Assessed at 1 or 24 hours after single dose Evaluate the inhibitory effect of MRX-2843 on MERTK phosphorylation in vivo JCI Insight. 2018 Nov 2;3(21):e97941

MRX-2843 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.20mL

10.23mL

2.05mL

1.02mL

20.46mL

4.09mL

2.05mL

MRX-2843 技术信息

CAS号1429882-07-4
分子式C29H40N6O
分子量 488.67
SMILES Code O[C@H]1CC[C@H](N2C=C(C3=CC=C(CN4CCN(C)CC4)C=C3)C5=CN=C(NCCC6CC6)N=C52)CC1
MDL No. MFCD28502224
别名 UNC2371
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

DMSO: 18 mg/mL(36.83 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 二
方案 三

Tags: MRX-2843 | 1429882-07-4 | UNC2371 | MRX2843 | MRX 2843 | UNC 2371 | UNC-2371 | MERTK/FLT3 Inhibitor | Protein Tyrosine Kinase/RTK | FLT3 | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | MRX-2843 纯度/质量文件 | MRX-2843 亚型比较 | MRX-2843 实验方案 | MRX-2843 技术信息

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