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抑制剂/激动剂
囊泡 肿瘤
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细胞凋亡
干细胞 MAPK/ERK Pathway 帕金森与阿尔茨海默症 肿瘤生长增殖和凋亡
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/ Ulixertinib

Ulixertinib {[allProObj[0].p_purity_real_show]}

货号：A162263 同义名： BVD-523;VRT752271 Ambeed 开学季，买赠积分，赢豪礼

Ulixertinib (BVD-523；VRT752271) 是一种强效、口服活性、高度选择性、ATP 竞争性和可逆的共价 ERK1/2 激酶抑制剂，对 ERK2 的 IC50 小于 0.3 nM。在 A375 黑色素瘤细胞系中，它抑制磷酸化的 ERK2 (pERK) 和下游激酶 RSK (pRSK)。

Ulixertinib 化学结构 CAS号：869886-67-9
Ulixertinib 化学结构
CAS号：869886-67-9
Ulixertinib 3D分子结构
CAS号：869886-67-9
Ulixertinib 化学结构 CAS号：869886-67-9
Ulixertinib 3D分子结构 CAS号：869886-67-9
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Ulixertinib 纯度/质量文件 产品仅供科研

货号：A162263 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 ERK ↓ ERK1 ↓ ERK2 ↓ ERK5 ↓ 其他靶点 纯度
DEL-22379 +

ERK, IC50: 0.5 μM

 		+

ERK, IC50: 0.5 μM

 		{[allProObj[0].p_purity_real_show]}
Pluripotin ++

ERK1, Kd: 98 nM

 		RasGAP {[allProObj[0].p_purity_real_show]}
FR 180204 +

ERK1, Ki: 0.31 μM

 		++

ERK2, Ki: 0.14 μM

 		{[allProObj[0].p_purity_real_show]}
Ravoxertinib +++

ERK1, IC50: 1.1 nM

 		++++

ERK2, IC50: 0.3 nM

 		{[allProObj[0].p_purity_real_show]}
SCH772984 +++

ERK1, IC50: 4 nM

 		++++

ERK2, IC50: 1 nM

 		{[allProObj[0].p_purity_real_show]}
Temuterkib +++

ERK1, IC50: 5 nM

 		+++

ERK2, IC50: 5 nM

 		{[allProObj[0].p_purity_real_show]}
VX-11e +++

ERK2, Ki: <2 nM

 		{[allProObj[0].p_purity_real_show]}
Ulixertinib ++++

ERK2, IC50: <0.3 nM

 		{[allProObj[0].p_purity_real_show]}
XMD17-109 ++

ERK5, IC50: 162 nM

 		{[allProObj[0].p_purity_real_show]}
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。

Ulixertinib 生物活性

靶点

  • ERK2

    ERK2, IC50:<0.3 nM
描述 ERK1/2 (extracellular-signal-regulated kinases) is only known substrates of the MEK1/2 as well as the essential node in RAS/RAF/MEK/ERK signaling cascade, which can be activated by catalyzing the phosphorylation on T202/Y204 through MEK1/2. Ulixertinib is a selective ERK1/2 inhibitor with IC50 value <0.3nM for ERK2, and Ki value of 0.3nM/0.04nM for ERK1/2[1][2]. The cellular study showed that Ulixertinib can inhibited p-ERK/p-RSK (the ERK substrate) with IC50 values of 4.1/0.14μM, as well as cell proliferation with IC50 value of 0.18μM of A375 cells[1]. Treatment with Ulixertinib at concentration of 2μM for 24h caused decrease of the ERK substrate, p-RSK, and the transcription targeted by ERK1/2, DUSP6, in BRAFV600E-mutant A375 melanoma cells. Meanwhile the increased p-ERK1/2 levels by this ATP-competitive inhibitor can also be observed. Ulixertinib at 0.25-4μM for 24h caused G1-arrested concentration-dependently in BRAFV600E-mutant melanoma cell line, UACC-62. A cell-line–dependent increase in caspase-3/7 by Ulixertinib was observed, as 3-fold greater induction of caspase-3/7 in a subset of cell lines with sensitivity to Ulixertinib (IC50<2μM). This could be further confirmed by attenuated p-RB and Cyclin D1, as well as the increased apoptotic marker BIM-EL by Ulixertinib in cells. Oral administration with Ulixertinib at 50 and 100mg/kg twice daily for 2 weeks suppressed tumor growth in A375 xenografts. The suppression of Colo205 tumors by Ulixertinib for 18 days could be observed at dose of 100mg/kg. Combination therapy with BVD-523 at dose of 100mg/kg with BRAF inhibitor dabrafenib (50mg/kg) can produce produced a 100% regression and a maximum 100% tumor growth delay in an A375 BRAFV600E-mutant melanoma model[2].
作用机制 Ulixertinib is an ATP-competitive ERK1/2 inhibitor. Notice that measuring increased pERK1/2 levels could be considered as a pharmacodynamic biomarker for Ulixertinib, though inhibition of ERK1/2 targets such as pRSK or DUSP6 could still be observed.[2]

Ulixertinib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
human A375 cells Function assay 2 h Inhibition of ERK1/2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-RSK level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis, IC50=0.14 μM 25977981
human A375 cells Proliferation assay 72 h Antiproliferative activity against human A375 cells harboring B-RAF V600E mutant after 72 hrs by Cellomics ArrayScanTM VTI imaging analysis, IC50=0.18 μM 25977981

Ulixertinib 动物研究

Dose Nude Mice: 5 mg/kg - 150 mg/kg[2] (p.o.) Rat: 10 mg/kg[3] (p.o.), 1 mg/kg[3] (i.v.)
Administration p.o., i.v.
Pharmacokinetics
Animal Mice[3] Rats[3] Dogs[3]
Dose 1 mg/kg (i.v.)
10 mg/kg (p.o.) 		1 mg/kg (i.v.)
10 mg/kg (p.o.) 		1 mg/kg (i.v.)
10 mg/kg (p.o.)
Administration i.v.
p.o. 		i.v.
p.o. 		i.v.
p.o.
F 91.6% (p.o.) 97.7% (p.o.) 33.8% (p.o.)
Vd 0.56 L/kg (i.v.) 0.36 ± 0.06 L/kg (i.v.) 1.61 L/kg (i.v.)
T1/2 1.04 h (i.v.)
2.06 h (p.o.) 		2.52 ± 0.07 h (i.v.)
2.02 ± 0.17 h (p.o.) 		1.21 h (i.v.)
1.29 h (p.o.)
Tmax 0.5 h (p.o.) 0.75 ± 0.29 h (p.o.) 2.00 h (p.o.)
CL 6.24 ml/min/kg (i.v.) 1.67 ± 0.25 ml/min/kg (i.v.) 15.5 ml/min/kg (i.v.)
AUC0→∞ 2672 ng·h/ml (i.v.)
24460 ng·h/ml (p.o.) 		10179 ± 1528 ng·h/ml (i.v.)
98421 ± 14005 ng·h/ml (p.o.) 		1091 ng·h/ml (i.v.)
3687 ng·h/ml (p.o.)
Cmax/C0 1918 ng/ml (i.v.)
7768 ng/ml (p.o.) 		6644 ± 1812 ng/ml (i.v.)
15,026 ± 2098 ng/ml (p.o.) 		1033 ng/ml (i.v.)
1442 ng/ml (p.o.)

Ulixertinib 参考文献

[1]Ward RA, Colclough N, et al. Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. J Med Chem. 2015 Jun 11;58(11):4790-801.

[2]Germann UA, Furey BF, et al. Targeting the MAPK Signaling Pathway in Cancer: Promising Preclinical Activity with the Novel Selective ERK1/2 Inhibitor BVD-523 (Ulixertinib). Mol Cancer Ther. 2017 Nov;16(11):2351-2363.

[3]Suresh PS, Jairam RK, et al. Prediction of Human Pharmacokinetics of Ulixertinib, a Novel ERK1/2 Inhibitor from Mice, Rats, and Dogs Pharmacokinetics. Eur J Drug Metab Pharmacokinet. 2018 Aug;43(4):453-460.

Ulixertinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.54mL

2.31mL

1.15mL

23.08mL

4.62mL

2.31mL

Ulixertinib 技术信息

CAS号869886-67-9
分子式C21H22Cl2N4O2
分子量 433.331
别名 BVD-523;VRT752271
运输蓝冰
存储条件

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 105 mg/mL(242.31 mM)，配合低频超声助溶，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
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 8 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

Tags: Ulixertinib | 869886-67-9 | BVD-523 | VRT752271 | BVD523 | BVD 523 | ERK1/2 Inhibitor | MAPK/ERK Pathway | Stem Cell/Wnt | ERK | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Ulixertinib 纯度/质量文件 | Ulixertinib 亚型比较 | Ulixertinib 生物活性 | Ulixertinib 细胞研究 | Ulixertinib 动物研究 | Ulixertinib 参考文献 | Ulixertinib 实验方案 | Ulixertinib 技术信息

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