Ulixertinib | BVD-523 | ERK1/2 Inhibitor | AmBeed-信号通路专用抑制剂

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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 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]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

ERK 亚型比较

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 BRAF_V600E-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 BRAF_V600E-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 BRAF_V600E-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.)
V_d	0.56 L/kg (i.v.)	0.36 ± 0.06 L/kg (i.v.)	1.61 L/kg (i.v.)
T_1/2	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.)
T_max	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.)
AUC_0→∞	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.)
C_max/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

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

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

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Ulixertinib 参考文献

Ulixertinib 实验方案

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