ERK-IN-1

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ERK-IN-1

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1715025-32-3

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
5mg	电议
10mg	电议
25mg	电议

产品介绍

ERK-IN-1（化合物 B）是一种可口服的 ERK1 和 ERK2 抑制剂，用于治疗以激活 MAPK 通路突变为特征的增殖性疾病。该活性尤其与 KRAS 突变 NSCLC、BRAF 突变 NSCLC、KRAS 突变胰腺癌、KRAS 突变结直肠癌 (CRC) 和 KRAS 突变卵巢癌的治疗有关。 ERK-IN-1 hydrochloride 也可以抑制 RAF。

Cas No.	1715025-32-3
Canonical SMILES	O=C(N[C@@H](C1=CC(F)=CC(Br)=C1)CNC)C2=CC=C(C3=NC([C@@H]4C[C@H](F)[C@@H](O)CC4)=CN=C3N)C=C2F
分子式	C₂₆H₂₇BrF₃N₅O₂
分子量	578.42
溶解度	Soluble in DMSO
储存条件	4°C, away from moisture and light
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	ERK-IN-1 (compound B) is a RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC (non-small celllung cancer), BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovanan cancer[1]. ERK-IN-1 (compound B) (50, 75 mg/kg, p.o., qd/q2d, 27 days) treatment significantly reduces the tumor volume in the Calu-6 human NSCLC subcutaneous tumor xenograft model in mice[1].\|\| Animal Model:\|Calu-6 NSCLC xenograft tumor models in mice[1].\|Dosage:\|50, 75 mg/kg.\|Administration:\|Orally either daily (qd) or every other day (q2d) for 27 days.\|Result:\|Significantly reduced the tumor volume. [1]. WO2018051306A1.