PF-07799933 (Claturafenib, ARRY-440) | mutant BRAF inhibitor

Chemical Structure : PF-07799933

CAS No.: 2754408-94-9

PF-07799933 (Claturafenib, ARRY-440, PF07799933, ARRY440)

Catalog No.: PC-22523Not For Human Use, Lab Use Only.

PF-07799933 (Claturafenib, ARRY-440) is a brain-penetrant, selective, pan-mutant BRAF inhibitor, demonstrated broad inhibition of pERK levels in cell lines harboring Class I (IC50=0.7-7 nM), II (10-14 nM), III (0.8, 7.8 nM), and indel (113, 179 nM) mutations, acquired BRAF p61 splice variant (59 nM), and acquired NRAS-Q61K (16 nM), but significantly spared pERK in BRAF wild-type cells (≥9800 nM).

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Biological Activity

PF-07799933 (Claturafenib, ARRY-440) is a brain-penetrant, selective, pan-mutant BRAF inhibitor, demonstrated broad inhibition of pERK levels in cell lines harboring Class I (IC50=0.7-7 nM), II (10-14 nM), III (0.8, 7.8 nM), and indel (113, 179 nM) mutations, acquired BRAF p61 splice variant (59 nM), and acquired NRAS-Q61K (16 nM), but significantly spared pERK in BRAF wild-type cells (≥9800 nM).

PF-07799933 (ARRY-440) disrupts endogenous mutant-BRAF:wild-type-CRAF dimers, and spares wild-type ERK signaling.

PF-07799933 (ARRY-440) inhibited pERK in vitro in cells driven by BRAF V600E-mutant monomers, BRAF Class II/III-mutant dimers, and treatment-acquired genetic alterations that induce mutant-BRAF V600E dimerization.

PF-07799933 disrupted endogenous mutant-BRAF:wild-type-CRAF dimers in cells containing BRAF V600E + p61 splice variant or BRAF V600E + NRAS Q61K that induce mutant BRAF dimerization.

PF-07799933 spared pERK and did not disrupt BRAF-wild-type:CRAF-wild-type dimers in vitro in BRAF wild-type cells.

PF-07799933 had broad in vivo anti-tumor activity, systemically and in the brain, against BRAF V600E and non-V600 mutations as monotherapy, and against BRAF V600E with a treatment-acquired BRAF p61 splice variant in combination with binimetinib.

Physicochemical Properties

M.Wt	490.31
Formula	C18H15Cl2F2N5O3S
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-(2-chloro-3-((5-chloro-3-methyl-4-oxo-3,4-dihydroquinazolin-6-yl)amino)-4-fluorophenyl)-3-fluoroazetidine-1-sulfonamide

References

1. Yaeger R, et al. Cancer Discov. 2024 Apr 30. doi: 10.1158/2159-8290.CD-24-0024.
2. US Patent Application No. 17/338,767 Ex. 126.

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PF-07799933 (Claturafenib, ARRY-440, PF07799933, ARRY440)

Biological Activity

Physicochemical Properties

References

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