2. Protein Tyrosine Kinase/RTK
  3. VEGFR FGFR
  4. CEP-11981

CEP-11981  (Synonyms: ESK981; BOL 303213X)

Cat. No.: HY-16135 Purity: 99.18%
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CEP-11981(ESK981; BOL 303213X) is an orally active tyrosine kinase inhibitor (TKI), which can target TIE2, VEGFR1-3 and FGFR1, and has potential anti-tumor and anti-angiogenic effects.

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

CEP-11981 Chemical Structure

CEP-11981 Chemical Structure

CAS No. : 856691-93-5

Size Price Stock Quantity
1 mg USD 350 In-stock
5 mg USD 980 In-stock
10 mg USD 1580 In-stock
25 mg USD 2980 In-stock
50 mg USD 4500 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of CEP-11981:

CEP-11981 Related Antibodies

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

View All Isoforms
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

View All FGFR Isoform Specific Products:

View All Isoforms
FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CEP-11981(ESK981; BOL 303213X) is an orally active tyrosine kinase inhibitor (TKI), which can target TIE2, VEGFR1-3 and FGFR1, and has potential anti-tumor and anti-angiogenic effects[1].

Cellular Effect
Cell Line Type Value Description References
HUVEC EC50
2 nM
Compound: 11b, CEP-11981
Antiangiogenic activity in HUVEC assessed as inhibition of capillary-tube formation by matrigel assay
Antiangiogenic activity in HUVEC assessed as inhibition of capillary-tube formation by matrigel assay
[PMID: 22148921]
In Vitro

CEP-11981(1μM, 72 h) can significantly inhibit the growth of RT4 cells[1].

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

CEP-11981 Related Antibodies
In Vivo

CEP-11981(2.5 mg/kg, 5 mg/kg or 10 mg/kg, oral gavage, daily, five days a week for two weeks) significantly arrested the growth of UC xenografts compared to control with no change in weight in murine xenograft model of RT4 human UC tumor[1].

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

477.56

Formula

C28H27N7O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC(C)CN(C1=C2C3=C(C(NC3)=O)C4=C1CCC5=NN(C)C=C54)C(C2=C6)=CC=C6NC7=NC=CC=N7
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 (104.70 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 2.0940 mL 10.4699 mL 20.9398 mL
5 mM 0.4188 mL 2.0940 mL 4.1880 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 2.0940 mL 10.4699 mL 20.9398 mL 52.3494 mL
5 mM 0.4188 mL 2.0940 mL 4.1880 mL 10.4699 mL
10 mM 0.2094 mL 1.0470 mL 2.0940 mL 5.2349 mL
15 mM 0.1396 mL 0.6980 mL 1.3960 mL 3.4900 mL
20 mM 0.1047 mL 0.5235 mL 1.0470 mL 2.6175 mL
25 mM 0.0838 mL 0.4188 mL 0.8376 mL 2.0940 mL
30 mM 0.0698 mL 0.3490 mL 0.6980 mL 1.7450 mL
40 mM 0.0523 mL 0.2617 mL 0.5235 mL 1.3087 mL
50 mM 0.0419 mL 0.2094 mL 0.4188 mL 1.0470 mL
60 mM 0.0349 mL 0.1745 mL 0.3490 mL 0.8725 mL
80 mM 0.0262 mL 0.1309 mL 0.2617 mL 0.6544 mL
100 mM 0.0209 mL 0.1047 mL 0.2094 mL 0.5235 mL
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CEP-11981 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:

CEP-11981856691-93-5ESK981 BOL 303213XCEP11981CEP 11981ESK 981ESK-981VEGFRFGFRVascular endothelial growth factor receptorFibroblast growth factor receptortyrosine kinaseTIE2VEGFR1-3FGFR1anti-tumoranti-angiogenicInhibitorinhibitorinhibit

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