Cat. No.: HY-16135

CEP-11981

(Synonyms: ESK981; BOL 303213X)

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Based on 1 Customer Validation

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.

Purity: 99.88%
CAS No.: 856691-93-5
Formula: C₂₈H₂₇N₇O
Molecular Weight:477.56

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CEP-11981 Chemical Structure

CAS No.: 856691-93-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

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].

All VEGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	20 μM Compound: 11b, CEP-11981	Inhibition of human Erg expressed CHO cells Inhibition of human Erg expressed CHO cells	[PMID: 22148921]
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]
HUVEC	EC₅₀	8 nM Compound: 11b, CEP-11981	Antiangiogenic activity in HUVEC assessed as inhibition of FGF-induced migration Antiangiogenic activity in HUVEC assessed as inhibition of FGF-induced migration	[PMID: 22148921]
HUVEC	EC₅₀	8 nM Compound: 11b, CEP-11981	Antiangiogenic activity in HUVEC assessed as inhibition of FGF-induced proliferation Antiangiogenic activity in HUVEC assessed as inhibition of FGF-induced proliferation	[PMID: 22148921]
HUVEC	EC₅₀	8 nM Compound: 11b, CEP-11981	Antiangiogenic activity in HUVEC assessed as inhibition of FGF-induced survival Antiangiogenic activity in HUVEC assessed as inhibition of FGF-induced survival	[PMID: 22148921]
HUVEC	EC₅₀	8 nM Compound: 11b, CEP-11981	Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced migration Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced migration	[PMID: 22148921]
HUVEC	EC₅₀	8 nM Compound: 11b, CEP-11981	Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced proliferation Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced proliferation	[PMID: 22148921]
HUVEC	EC₅₀	8 nM Compound: 11b, CEP-11981	Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced survival Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced survival	[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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 856691-93-5
Appearance Solid
Molecular Weight 477.56
Formula C₂₈H₂₇N₇O
Color 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
Synonyms

ESK981; BOL 303213X
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0940 mL

10.4699 mL

20.9398 mL

5 mM

0.4188 mL

2.0940 mL

4.1880 mL

10 mM

0.2094 mL

1.0470 mL

2.0940 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Weiguo Jian, et al. The angiopoietin-TIE2 pathway is a potential therapeutic target in urothelial carcinoma. Anticancer Res. 2014 Jul;34(7):3377-82. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

All VEGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

CEP-11981

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

All VEGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

CEP-11981 Related Classifications

HY-16135 Related Classifications