Rineterkib(ERK-IN-1;compound B) chemical structure
Chemical structureResearch use only
CAT. NO. DC57035Featured

Rineterkib(ERK-IN-1;compound B)

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TotalUS$850
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Product overview

Description & Application

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].

ParameterValue
Chemical NameRineterkib free base
CAS No.1715025-32-3
SynonymsRineterkib;LTT-462;LTT 462;LTT462
FormulaC26H27BrF3N5O2
M.Wt578.434
SMILESN(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.

Product documentation

Refer to the certificate supplied with your lot for batch-specific release results.

Handling guide

-20

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