2. Cell Cycle/DNA Damage Cytoskeleton Metabolic Enzyme/Protease Stem Cell/Wnt JAK/STAT Signaling
  3. Microtubule/Tubulin HIF/HIF Prolyl-Hydroxylase STAT
  4. ENMD-1198

ENMD-1198  (Synonyms: IRC-110160)

Cat. No.: HY-16196 Purity: 98.06%
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ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.

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

ENMD-1198 Chemical Structure

ENMD-1198 Chemical Structure

CAS No. : 864668-87-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1713 In-stock
Solution
10 mM * 1 mL in DMSO USD 1713 In-stock
Solid
1 mg USD 500 In-stock
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10 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

ENMD-1198 Related Antibodies

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HIF-1α HIF

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STAT3 STAT5 STAT6 STAT1

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Description

ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.

IC50 & Target[3]

STAT3

 

HIF-1α

 

In Vitro

ENMD-1198 (0-5 μM; 24 hours) leads to a significant dose-dependent inhibition of HCC cell growth with IC50s of 2.5 μM for HUH-7 and HepG2 cells, respectively[3].
ENMD-1198 (2.5 μM; 16 hours) abrogates EGF-induced phosphorylation of Akt (HUH-7), FAK (HUH-7), p44/42 MAPK (HepG2), and STAT3 (HUH-7, HepG2)[3].

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

ENMD-1198 Related Antibodies

Cell Viability Assay[3]

Cell Line: HUH-7 and HepG2 cells
Concentration: 0-5 μM
Incubation Time: 24 hours
Result: Led to a significant dose-dependent inhibition of HCC cell growth.

Western Blot Analysis[3]

Cell Line: HUH-7 and HepG2 cells
Concentration: 2.5 μM
Incubation Time: 16 hours
Result: Abrogated EGF-induced phosphorylation of Akt (HUH-7), FAK (HUH-7), p44/42 MAPK (HepG2), and STAT3 (HUH-7, HepG2).
In Vivo

ENMD-1198 (200 mg/kg; p.o.; daily from day 7 to day 19) effectively inhibits growth of hepatocellular carcinoma through direct effects on the tumor cells, and also through inhibition of angiogenesis[3].

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

Animal Model: Eight-week-old male athymic nude mice (BALB/c nu/nu) (xenografted hepatocellular tumors)[3]
Dosage: 200 mg/kg
Administration: P.o.; daily from day 7 to day 19
Result: Led to a significant growth inhibition of xenografted hepatocellular tumors.
Molecular Weight

311.42

Formula

C20H25NO2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

C[C@@]12C=CC[C@@]1([H])[C@]3([H])CCC4=C(C=C(OC)C(C(N)=O)=C4)[C@@]3([H])CC2
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 : 100 mg/mL (321.11 mM; Need ultrasonic and warming; 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 3.2111 mL 16.0555 mL 32.1110 mL
5 mM 0.6422 mL 3.2111 mL 6.4222 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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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: 2.5 mg/mL (8.03 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (8.03 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 3.2111 mL 16.0555 mL 32.1110 mL 80.2774 mL
5 mM 0.6422 mL 3.2111 mL 6.4222 mL 16.0555 mL
10 mM 0.3211 mL 1.6055 mL 3.2111 mL 8.0277 mL
15 mM 0.2141 mL 1.0704 mL 2.1407 mL 5.3518 mL
20 mM 0.1606 mL 0.8028 mL 1.6055 mL 4.0139 mL
25 mM 0.1284 mL 0.6422 mL 1.2844 mL 3.2111 mL
30 mM 0.1070 mL 0.5352 mL 1.0704 mL 2.6759 mL
40 mM 0.0803 mL 0.4014 mL 0.8028 mL 2.0069 mL
50 mM 0.0642 mL 0.3211 mL 0.6422 mL 1.6055 mL
60 mM 0.0535 mL 0.2676 mL 0.5352 mL 1.3380 mL
80 mM 0.0401 mL 0.2007 mL 0.4014 mL 1.0035 mL
100 mM 0.0321 mL 0.1606 mL 0.3211 mL 0.8028 mL
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ENMD-1198 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:

ENMD-1198864668-87-1IRC-110160ENMD1198ENMD 1198IRC110160IRC 110160Microtubule/TubulinHIF/HIF Prolyl-HydroxylaseSTATHypoxia-inducible factorsHIFsHIF-PHhepatocellularcarcinomacellsHUH-7HepG2vascularizationInhibitorinhibitorinhibit

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