1. MAPK/ERK Pathway
    Protein Tyrosine Kinase/RTK
    Cell Cycle/DNA Damage
  2. Raf
    VEGFR
    PERK
  3. Takeda-6D

Takeda-6D 

Cat. No.: HY-18318
Handling Instructions

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.

For research use only. We do not sell to patients.

Takeda-6D Chemical Structure

Takeda-6D Chemical Structure

CAS No. : 1125632-93-0

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Description

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

VEGFR2

2.2 nM (IC50)

Braf

7.0 nM (IC50)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

547.99

Formula

C27H19ClFN5O3S

CAS No.
SMILES

O=C(NC1=CC(OC2=CC=C3C(SC(NC(C4CC4)=O)=N3)=N2)=CC=C1F)C5=CC=CC(C6(C#N)CC6)=C5Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Takeda-6D
Cat. No.:
HY-18318
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