Takeda-6D


CAS No. : 1125632-93-0

1125632-93-0
Price and Availability of CAS No. : 1125632-93-0
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Cat. No. : HY-18318
M.Wt: 547.99
Formula: C27H19ClFN5O3S
Purity: >98 %
Solubility: 10 mM in DMSO
Introduction of 1125632-93-0 :

Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity[1]. IC50 & Target: IC50: 2.2 nM (VEGFR2), 7.0 nM (BRAF)[1] In Vivo: Takeda-6D (compound 6d) (10 mg/kg, Orally, once) shows sufficient oral bioavailability (F = 70.5%) in rats[1].
Takeda-6D (0-10 mg/kg, Orally, once) significantly decreases phosphorylation levels of ERK1/24 h after oral administration in an A375 (BRAFV600E mutant) human melanoma xenograft model in rats[1].
Takeda-6D (10 mg/kg, Orally, twice daily for 2 weeks) shows tumor regression with T/Cof ?7.0% without severe toxicity, and this tumor regression should include the efficacy based on the antiangiogenesis potency and BRAF inhibitory activity[1].

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