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/ Ulixertinib

Ulixertinib {[allProObj[0].p_purity_real_show]}

货号：A162263 同义名： BVD-523; VRT752271

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

 		98%
Pluripotin ++

ERK1, Kd: 98 nM

 		RasGAP 98+%
FR 180204 +

ERK1, Ki: 0.31 μM

 		++

ERK2, Ki: 0.14 μM

 		98%
Ravoxertinib +++

ERK1, IC50: 1.1 nM

 		++++

ERK2, IC50: 0.3 nM

 		99%+
SCH772984 +++

ERK1, IC50: 4 nM

 		++++

ERK2, IC50: 1 nM

 		99%+
Temuterkib +++

ERK1, IC50: 5 nM

 		+++

ERK2, IC50: 5 nM

 		99%+
VX-11e +++

ERK2, Ki: <2 nM

 		99%+
Ulixertinib ++++

ERK2, IC50: <0.3 nM

 		99%+
XMD17-109 ++

ERK5, IC50: 162 nM

 		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。

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 细胞实验

Cell Line
Concentration Treated Time Description References
QBC939 cells 1 µM 24 h To investigate the effect of the ERK inhibitor ulixertinib on the proliferation and migration of QBC939 cells. Results showed that ERK inhibition could suppress the promotion of proliferation and migration induced by SPRY4 knockdown. EBioMedicine. 2019 Dec;50:166-177.
QBC939 cells 1 µM 24 h To investigate the effect of ulixertinib on the cell cycle distribution of QBC939 cells. Results showed that ulixertinib increased the percentage of cells in the G1 phase and decreased the percentage of cells in the S and G2/M phases. EBioMedicine. 2019 Dec;50:166-177.
OMM2.3 cells 2 μM 72 h To evaluate the anti-proliferative effect of Ulixertinib in combination with BIX01294 on OMM2.3 cells, the results showed that the combination significantly enhanced the anti-proliferative effect. Acta Pharm Sin B. 2024 Mar;14(3):1187-1203.

Ulixertinib 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice QBC939 cell xenograft model Intraperitoneal injection 3 mg/kg Once daily for 15 days To investigate the effect of FGF2 stimulation on the SPRY4-overexpressing QBC939 cell xenograft model. Results showed that SPRY4 overexpression repressed tumor volume and weight, while FGF2 addition reversed this effect. EBioMedicine. 2019 Dec;50:166-177.
Mice ES2 xenograft model Intraperitoneal injection 50 mg/kg Every other day for three weeks To evaluate the effect of ERK inhibition on tumor progression, results showed that Ulixertinib significantly slowed tumor growth J Biomed Sci. 2023 Dec 9;30(1):94
Nude mice UM orthotopic model Oral 50 mg/kg Once daily for 21 days To evaluate the inhibitory effect of Ulixertinib alone and in combination with UNC0631 on UM tumor growth, the results showed that the combination significantly inhibited tumor growth. Acta Pharm Sin B. 2024 Mar;14(3):1187-1203.

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 433.33
SMILES Code O=C(C1=CC(C2=CC(NC(C)C)=NC=C2Cl)=CN1)N[C@@H](C3=CC=CC(Cl)=C3)CO
MDL No. MFCD22628898
别名 BVD-523; VRT752271
运输蓝冰
InChI Key KSERXGMCDHOLSS-LJQANCHMSA-N
Pubchem ID 11719003
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C
溶解方案

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

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
方案 四
配制的工作液建议现用现配，短期内尽快用完。 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

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 动物研究 | Ulixertinib 参考文献 | Ulixertinib 实验方案 | Ulixertinib 技术信息

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