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

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.

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Takeda-6D

Takeda-6D Chemical Structure

CAS No. : 1125632-93-0

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Based on 1 publication(s) in Google Scholar

Takeda-6D Related Antibodies

Top Publications Citing Use of Products

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B-Raf C-Raf Raf

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

547.99

Formula

C27H19ClFN5O3S
CAS No.
Appearance

Solid

Color

White to light yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (91.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8249 mL 9.1243 mL 18.2485 mL
5 mM 0.3650 mL 1.8249 mL 3.6497 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8249 mL 9.1243 mL 18.2485 mL 45.6213 mL
5 mM 0.3650 mL 1.8249 mL 3.6497 mL 9.1243 mL
10 mM 0.1825 mL 0.9124 mL 1.8249 mL 4.5621 mL
15 mM 0.1217 mL 0.6083 mL 1.2166 mL 3.0414 mL
20 mM 0.0912 mL 0.4562 mL 0.9124 mL 2.2811 mL
25 mM 0.0730 mL 0.3650 mL 0.7299 mL 1.8249 mL
30 mM 0.0608 mL 0.3041 mL 0.6083 mL 1.5207 mL
40 mM 0.0456 mL 0.2281 mL 0.4562 mL 1.1405 mL
50 mM 0.0365 mL 0.1825 mL 0.3650 mL 0.9124 mL
60 mM 0.0304 mL 0.1521 mL 0.3041 mL 0.7604 mL
80 mM 0.0228 mL 0.1141 mL 0.2281 mL 0.5703 mL
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Takeda-6D Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Takeda-6D1125632-93-0RafVEGFRPERKRaf kinasesVascular endothelial growth factor receptorProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseantiangiogenesisHUVEC cellsantitumorpERKRAForally activeInhibitorinhibitorinhibit

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