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Chemical Structure : PF-07284890
CAS No.: 2573781-75-4
Catalog No.: PC-72612Not For Human Use, Lab Use Only.
Tinlorafenib (PF-07284890, ARRY-461) is an orally bioavailable, brain penetrant, potent, small molecule BRAF V600 mutants inhibitor, inhibits BRAF and CRAF with IC50 of 5.8 and 4.1 nM, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $258 | In stock | |
| 10 mg | $428 | In stock | |
| 25 mg | $728 | In stock | |
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Tinlorafenib (PF-07284890, ARRY-461) is an orally bioavailable, brain penetrant, potent, small molecule BRAF V600 mutants inhibitor, inhibits BRAF and CRAF with IC50 of 5.8 and 4.1 nM, respectively.
PF-07284890 inhibits the clinically relevant kinase domain BRAF V600 mutants (V600E and V600K) with IC50 of 24-25 nM.
PF-07284890 potently inhibits phosphorylation of ERK, a downstream marker of BRAF inhibition, and potently inhibits proliferation of BRAF V600E/K mutant melanoma cell lines (IC50=18-38 nM).
PF-07284890 inhibits phosphorylation of ERK in A375 BRAF V600E tumors, achieving maximal target inhibitions at a dose of 10 mg/kg.
PF-07284890 (10-30 mg/kg BID) caused significant and durable tumor regressions in the intracranial A375-luc BRAF V600E melanoma xenograft model.
| M.Wt | 456.89 | |
| Formula | C19H19ClF2N4O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO (4.6 mg/mL) |
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| Chemical Name/SMILES |
N-[2-Chloro-3-[(3,4-dihydro-3,5-dimethyl-4-oxo-6-quinazolinyl)amino]-4-fluorophenyl]-3-fluoro-1-propanesulfonamide |
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1. Patent WO2020261156A1.
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