Rineterkib(ERK-IN-1;compound B) Datasheet | DC57035

Rineterkib(ERK-IN-1;compound B) — Datasheet

CAT. NO. DC57035

Parameter	Value
Chemical Name	Rineterkib free base
CAS No.	1715025-32-3
Synonyms	Rineterkib;LTT-462;LTT 462;LTT462
Formula	C26H27BrF3N5O2
M.Wt	578.434
SMILES	N(C(C1C=CC(C2C(N)=NC=C([C@H]3CC[C@@H]([C@H](C3)F)O)N=2)=CC=1F)=O)[C@H](CNC)C1C=C(C=C(C=1)Br)F
Purity	>98%
Storage	-20

Biological Activity

Rineterkib(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].

In Vitro

No in vitro data are provided in the current product source. Contact us for further information.

In Vivo

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.

Target

RAF

ERK1

ERK2

References & source

[1]. WO2018051306A1.

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.