[CAS NO. 1207293-36-4]  BI-847325

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PRODUCTS SPECIFICATIONS [1207293-36-4]

Distributor
Catalog
SLK-S7843
Brand
Selleck
CAS
1207293-36-4

DESCRIPTION [1207293-36-4]

Overview

MDLMFCD28978743
Molecular Weight464.56
Molecular FormulaC29H28N4O2
SMILESO=C(NCC)C#CC1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=C(CN(C)C)C=C3)/C4=CC=CC=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.1526 mL10.7629 mL21.5257 mL
5 mM0.4305 mL2.1526 mL4.3051 mL
10 mM0.2153 mL1.0763 mL2.1526 mL
50 mM---

Description

BI-847325 is an orally bioavailable, and selective dual inhibitor with of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.

Targets

Aurora B (Xenopus laevis) [1]MEK2 [1]Aurora C (Human) [1]Aurora A (Human) [1]MEK1 [1]
3 nM4 nM15 nM25 nM25 nM

In vitro

BI-847325 shows growth-inhibitory effects on BRAF-mutant and vemurafenib-resistant melanoma cells with IC50 ranging from 0.3 nM to 2 μM, and prevents colony formation in six BRAF-mutant melanoma cell lines. BI-847325 also induces apoptosis by reducing Mcl-1 expression.

In vivo

In mice bearing 1205Lu and 1205LuR xenografts, BI-847325 (75 mg/kg, p.o.) causes significant tumor suppression without significant alteration in the body weights.