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Referencia número: HY-164492

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LSN3074753

LSN3074753, an analog of LY3009120 (HY-12558), is a pan-RAF and Raf dimer inhibitor. LSN3074753 demonstrates activity against tumor cells with MAPK pathway activation driven by BRAF monomer or RAF dimers including BRAF- or KRAS-mutant colorectal cancer. LSN3074753 combined with Cetuximab (HY-P9905) shows additive and synergistic effects for colorectal cancer PDX models, particularly those with KRAS or BRAF mutation.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS: 1455031-68-1
Fòrmula: C₂₄H₃₀FN₅O₂
Peso molecular:439.53

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (266 KB)

LSN3074753 Chemical Structure

No. CAS: 1455031-68-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
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- Cellular Effect
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Actividad biológica

Descripciòn

Ver todos los productos específicos de isoformas Raf :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	ED₅₀	1.7 mg/kg Compound: 6	In vivo inhibition of BRAF V600E mutant in human A375 cells xenografted in po dosed athymic nu/nu mouse assessed as inhibition of ERK phosphorylation by ELISA In vivo inhibition of BRAF V600E mutant in human A375 cells xenografted in po dosed athymic nu/nu mouse assessed as inhibition of ERK phosphorylation by ELISA	[PMID: 25965804]
A-375	IC₅₀	0.01 μM Compound: 6	Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay	[PMID: 25965804]
A-375	IC₅₀	0.022 μM Compound: 6	Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay	[PMID: 25965804]
HCT-116	IC₅₀	0.16 μM Compound: 6	Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA	[PMID: 25965804]
HCT-116	IC₅₀	0.174 μM Compound: 6	Antiproliferative activity against human HCT116 cells after 67 hrs by resazurin assay Antiproliferative activity against human HCT116 cells after 67 hrs by resazurin assay	[PMID: 25965804]

Chemical Information

No. CAS 1455031-68-1
Peso molecular 439.53
Fòrmula C₂₄H₃₀FN₅O₂
SMILES

O=C(NC[C@@H](O)C(C)(C)C)NC1=CC(C2=CC3=CN=C(NC)C=C3N=C2C)=C(C)C=C1F
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (266 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Yao YM, et al. Mouse PDX Trial Suggests Synergy of Concurrent Inhibition of RAF and EGFR in Colorectal Cancer with BRAF or KRAS Mutations. Clin Cancer Res. 2017 Sep 15;23(18):5547-5560. [Content Brief]

[2]. Sorokin A, et al. Antitumor activity of panRAF inhibition in BRAF V600E metastatic colorectal cancer[J]. 2017.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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LSN3074753

Ver todos los productos específicos de isoformas Raf

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

LSN3074753 Related Classifications

HY-164492 Related Classifications