ENMD-1198 (Synonyms: IRC-110160)

Name: ENMD-1198
Brand: MedChemExpress
SKU: HY-16196
Rating: 4.5 (1 reviews)

Cat. No.: HY-16196 Purity: 98.06%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 864668-87-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 753	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 753	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 685	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1100	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2200	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 3500	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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HIF-1α HIF

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STAT3 STAT5 STAT6 STAT1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[3]

STAT3

HIF-1α

Cellular Effect

Cell Line	Type	Value	Description	References
HUVEC	IC₅₀	0.13 μM Compound: 9d	Antiangiogenic activity against HUVEC assessed as growth inhibition after 48 hrs by WST1 assay Antiangiogenic activity against HUVEC assessed as growth inhibition after 48 hrs by WST1 assay	[PMID: 19782564]
MDA-MB-231	IC₅₀	0.2 μM Compound: 9d	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by WST1 assay Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by WST1 assay	[PMID: 19782564]

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.

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.

864668-87-1

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
10 mM	0.3211 mL	1.6055 mL	3.2111 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (8.03 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 98.87%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (249 KB) HNMR (96 KB) RP-HPLC (90 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[1]. Pasquier E, et al. ENMD-1198, a new analogue of 2-methoxyestradiol, displays both antiangiogenic and vascular-disrupting properties. Mol Cancer Ther. 2010 May;9(5):1408-18. [Content Brief]

[2]. Snoeks TJ, et al. 2-methoxyestradiol analogue ENMD-1198 reduces breast cancer-induced osteolysis and tumor burden both in vitro and in vivo. Mol Cancer Ther. 2011 May;10(5):874-82. [Content Brief]

[3]. Moser C, et al. ENMD-1198, a novel tubulin-binding agent reduces HIF-1alpha and STAT3 activity in human hepatocellular carcinoma(HCC) cells, and inhibits growth and vascularization in vivo. BMC Cancer. 2008 Jul 23;8:206. [Content Brief]

Complete Stock Solution Preparation Table

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

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.

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ENMD-1198 (Synonyms: IRC-110160)

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ENMD-1198 Related Antibodies

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References

Customer Review

ENMD-1198 Related Antibodies

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Complete Stock Solution Preparation Table

ENMD-1198 Related Classifications

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