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Rineterkib(ERK-IN-1;compound B)

  Cat. No.:  DC57035   Featured
Chemical Structure
1715025-32-3
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Field of application
Rineterkib, also known as LTT-462 or ERK-IN-1, is a RAF and ERK1/2 inhibitor which has demonstrated preclinical activity in multiple MAPK activated cancer cells and xenograft models. LTT462 binds to and inhibits ERK, thereby preventing the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is upregulated in numerous tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1715025-32-3
Chemical Name: Rineterkib free base
Synonyms: Rineterkib;LTT-462;LTT 462;LTT462
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
Formula: C26H27BrF3N5O2
M.Wt: 578.434
Purity: >98%
Sotrage: -20
Description: 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].
Target: RAF ERK1 ERK2
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.
References: [1]. WO2018051306A1.
MSDS
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