LXH254 |CAS:1800398-38-2 Probechem Biochemicals

Chemical Structure : LXH254

CAS No.: 1800398-38-2

LXH254 (Naporafenib, LXH-254)

Catalog No.: PC-35635Not For Human Use, Lab Use Only.

LXH254 (Naporafenib, LXH 254) is a highly potent, selective B/C RAF inhibitor with Kd of 1.3/3.6 nM respectively, shows less activity against ARAF.

Packing	Price	Stock
5 mg	$118	In stock
10 mg	$198	In stock
25 mg	$328	In stock
50 mg	$528	In stock
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Biological Activity

LXH254 (Naporafenib, LXH 254) is a highly potent, selective B/C RAF inhibitor with Kd of 1.3/3.6 nM respectively, shows less activity against ARAF.

LXH254 (Naporafenib) inhibits pMEK and cell proliferation in Calu-6 cells with EC50 of 0.014 uM and 0.47 uM, respectively

LXH254 (Naporafenib) showed a high level of selectivity on a panel of 456 kinases, demonstrating greater than 98% on-target binding to BRAF, BRAFV600E, and CRAF at 1 uM and very few off-targets, with DDR1 (>99%), DDR2 (84%), and PDGFRb (>99%) the only kinases with binding >80% at 1 uM.

LXH254 (Naporafenib) was active in models harboring BRAF alterations, including atypical BRAF alterations coexpressed with mutant K/NRAS, and NRAS mutants, but had only modest activity in KRAS mutants. LXH254 caused paradoxical activation of MAPK signaling in a manner similar to dabrafenib in cells expressing only ARAF.

LXH254 (Naporafenib) demonstrated tumor regression in the Calu-6 xenograft nude rat model.

Physicochemical Properties

M.Wt	502.494
Formula	C25H25F3N4O4
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide

References

1. Monaco KA, et al. Clin Cancer Res. 2021 Apr 1;27(7):2061-2073.
2. Ramurthy S, et al. J Med Chem. 2020 Mar 12;63(5):2013-2027.
3. Negrao MV, et al. J Thorac Oncol. 2020 Oct;15(10):1611-1623.

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LXH254 (Naporafenib, LXH-254)

Biological Activity

Physicochemical Properties

References

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