|(S)-4-(5-氯-2-(异丙胺基)吡啶-4-基)-N-(1-(3-氯苯基)-2-羟乙基)-1H-吡咯-2-酰胺盐酸盐|CsnPharm

CAS No.: 1956366-10-1

(S)-4-(5-Chloro-2-(isopropylamino)pyridin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide hydrochloride Catalog No. CSN23392

Synonyms: BVD-523 hydrochloride;VRT752271 hydrochloride;Ulixertinib (hydrochloride)

Ulixertinib HCl, the salt of ulixertinib, is a reversible inhibitor of ERK1/ERK2. It can inhibit cell proliferation.

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技术信息

生物活性

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 HCl is the hydrochloride form of Ulixertinib. 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. 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. 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1286 mL
- 10.6430 mL
- 21.2860 mL
- 5 mM
- 0.4257 mL
- 2.1286 mL
- 4.2572 mL
- 10 mM
- 0.2129 mL
- 1.0643 mL
- 2.1286 mL

技术信息

CAS号

1956366-10-1

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H23Cl3N4O2

运输

蓝冰

分子量

469.79

别名

BVD-523 hydrochloride;VRT752271 hydrochloride;Ulixertinib (hydrochloride);BVD-523;VRT-752271

溶解度

DMSO	120.0 mg/mL (255.4 mM) warming
Water	Insoluble

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(S)-4-(5-Chloro-2-(isopropylamino)pyridin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide hydrochloride Catalog No. CSN23392

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