Takeda-6d
Modify Date: 2024-01-04 17:50:25
Takeda-6d structure
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Common Name | Takeda-6d | ||
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| CAS Number | 1125632-93-0 | Molecular Weight | 547.988 | |
| Density | 1.6±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C27H19ClFN5O3S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Takeda-6dTakeda-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]. |
| Name | 2-chloro-3-(1-cyanocyclopropyl)-N-(5-((2-(cyclopropanecarboxamido)thiazolo[5,4-b]pyridin-5-yl)oxy)-2-fluorophenyl)benzamide |
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| Synonym | More Synonyms |
| 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]. |
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| Related Catalog | |
| 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]. |
| References |
| Density | 1.6±0.1 g/cm3 |
|---|---|
| Molecular Formula | C27H19ClFN5O3S |
| Molecular Weight | 547.988 |
| Exact Mass | 547.088135 |
| PSA | 145.24000 |
| LogP | 3.83 |
| Index of Refraction | 1.725 |
| Benzamide, 2-chloro-3-(1-cyanocyclopropyl)-N-[5-[[2-[(cyclopropylcarbonyl)amino]thiazolo[5,4-b]pyridin-5-yl]oxy]-2-fluorophenyl]- |
| 2-Chloro-3-(1-cyanocyclopropyl)-N-[5-({2-[(cyclopropylcarbonyl)amino][1,3]thiazolo[5,4-b]pyridin-5-yl}oxy)-2-fluorophenyl]benzamide |