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LXH254

Catalog No. T11898 CAS 1800398-38-2

LXH254 is a potent C-Raf and B-Raf inhibitor.

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LXH254, CAS 1800398-38-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 48.00
5 mg	In stock	$ 124.00
10 mg	In stock	$ 195.00
25 mg	In stock	$ 382.00
50 mg	In stock	$ 597.00
100 mg	In stock	$ 726.00
200 mg	In stock	$ 997.00
500 mg	In stock	$ 1,520.00
1 mL * 10 mM (in DMSO)	In stock	$ 137.00

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Purity: 99.92%

Purity: 99.45%

Purity: 99.31%

Purity: 98.3%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	LXH254 is a potent C-Raf and B-Raf inhibitor.
Targets&IC50	BRAF:0.21 nM (IC50), Raf:0.072 nM (IC50), Abl-1:4.9 μM (IC50), ARAF:6.4 nM (IC50), p38α:2.1 μM (IC50)
In vitro	LXH254 is an adenosine triphosphate (ATP)-competitive inhibitor of BRAF and CRAF protein kinases. LXH254 is also referred to as a c-RAF (or CRAF) inhibitor or a C-RAF/c-Raf kinase inhibitor. In cell-based assays, LXH254 has demonstrated anti-proliferative activity in cell lines that contain a variety of mutations that activate MAPK signaling. Moreover, LXH254 is a Type 2 ATP -competitive inhibitor of both B-Raf and C-Raf that keeps the kinase pocket in an inactive conformation, thereby reducing the paradoxical activation seen with many B-Raf inhibitors, and blocking mutant RAS-driven signaling and cell proliferation.
In vivo	LXH254 exhibits efficacy in numerous MAPK-driven human cancer cell lines and in xenograft tumors representing model tumors harboring human lesions in KRAS, NRAS and BRAF oncogenes.Treatment with LXH254 generates tumor regression in several KRAS-mutant models including the NSCLC-derived Calu-6 (KRAS Q61K) and NCI-H358 (KRAS G12C).

Molecular Weight	502.49
Formula	C25H25F3N4O4
CAS No.	1800398-38-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (199.01 mM), Sonification is recommended.

References and Literature

1. CAPONIGRO, Giordano, et al. THERAPEUTIC COMBINATIONS COMPRISING A RAF INHIBITOR AND A ERK INHIBITOR. WO 2018051306 A1 20180322

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Highly Selective Inhibitor Library Anti-Cancer Drug Library Inhibitor Library Anti-Liver Cancer Compound Library Anti-Ovarian Cancer Compound Library ReFRAME Related Library

Related Products

Related compounds with same targets

Regorafenib Raf inhibitor 3 RMC-0331 Lifirafenib Agerafenib Lonafarnib Vem-L-Cy5 OSI-930

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

LXH254 1800398-38-2 MAPK Raf Bcr-Abl A375 Inhibitor p38 MAPK inhibit Mia PaCa-2 Raf kinases LXH-254 LXH 254 HCT116 Selective MEL-JUSO inhibitor

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