Larotinib mesylate hydrate is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC 50 of 0.6 nM In Vivo After daily administration of Larotinib mesylate hydrate, the no observed adverse effect level (NOAEL) is 10 mg/kg in Sprague-Dawley rats and the lowest observed adverse effect level (LOAEL) is 5 mg/kg in beagle dogs. The maximal tolerable doses (MTDs) are 20 and 25 mg/kg in Sprague-Dawley rats and beagle dogs, respectively . Larotinib mesylate hydrate shows dose-dependent antitumor results and a tumor-inhibiting rate exceeding 60% at 18 mg/kg in a tumor-bearing mice model (data not published) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:EGFR L861Q 0.423 nM (IC 50 ) EGFR L858R 0.563 nM (IC 50 ) EGFR (WT) 0.611 nM (IC 50 ) EGFR T790M 45.2 nM (IC 50 ) HER4 84 nM (IC 50 ) BLK 102 nM (IC 50 ) IRAK-1 167 nM (IC 50 ) BTK 196 nM (IC 50 ) HER2 253 nM (IC 50 )
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Larotinib mesylate hydrate
CAS number：2097129-93-4 molecular formula：C26H36ClFN4O11S2
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| Chinese alias | 拉罗替尼甲磺酸盐水合物 | ||
| English alias | - | ||
| CAS number | 2097129-93-4 | molecular formula | C26H36ClFN4O11S2 |
| molecular weight | 699.17 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
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