I-OMe-Tyrphostin AG 538 (Synonyms: I-OMe-AG 538)

Name: I-OMe-Tyrphostin AG 538
Brand: MedChemExpress
SKU: HY-135680
Rating: 4.5 (1 reviews)

Cat. No.: HY-135680 Purity: 98.03%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC₅₀ of 1 µM.

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

I-OMe-Tyrphostin AG 538 Chemical Structure

CAS No. : 1094048-77-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 165	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 165	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1350	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

IC₅₀ & Target

IC50: 1 µM (PI5P4Kα)^[1]

In Vitro

I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) (0.1-1000 µM; 24 hours) is cytotoxic to PANC-1 cells in nutrient-deprived medium^[1].
I-OMe-Tyrphostin AG 538 (0-3 µM; 1 hour) blocks phosphorylation of IGF-1R, Akt and Erk^[1].

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

Cell Viability Assay^[1]

Cell Line:	PANC-1 cells
Concentration:	0.1, 1, 10, 1000 µM
Incubation Time:	24 hours
Result:	Cytotoxic to PANC-1 cells in nutrient-deprived medium.

Western Blot Analysis^[1]

Cell Line:	PANC-1 cells (stimulation with 50 ng/ml IGF-1 for 10 min)
Concentration:	0.03, 0.3, 3 µM
Incubation Time:	1 hour
Result:	Blocked phosphorylation of IGF-1R, Akt and Erk.

Molecular Weight

437.19

Formula

C₁₇H₁₂INO₅

CAS No.

1094048-77-7

Appearance

Solid

Color

Yellow to orange

SMILES

N#C/C(C(C1=CC=C(O)C(O)=C1)=O)=C\C2=CC(OC)=C(O)C(I)=C2

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 (114.37 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	2.2873 mL	11.4367 mL	22.8734 mL
5 mM	0.4575 mL	2.2873 mL	4.5747 mL
10 mM	0.2287 mL	1.1437 mL	2.2873 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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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 (5.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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 (5.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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)

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: 98.03%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (247 KB) HNMR (259 KB) RP-HPLC (247 KB) MS (68 KB)

Handling Instructions (2659 KB)

References

[1]. Davis MI, et al. A homogeneous, high-throughput assay for phosphatidylinositol 5-phosphate 4-kinase with a novel, rapid substrate preparation. PLoS One. 2013;8(1):e54127. [Content Brief]

[2]. Momose I, et al. Inhibitors of insulin-like growth factor-1 receptor tyrosine kinase are preferentially cytotoxic to nutrient-deprived pancreatic cancer cells. Biochem Biophys Res Commun. 2009 Feb 27;380(1):171-6. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2873 mL	11.4367 mL	22.8734 mL	57.1834 mL
	5 mM	0.4575 mL	2.2873 mL	4.5747 mL	11.4367 mL
	10 mM	0.2287 mL	1.1437 mL	2.2873 mL	5.7183 mL
	15 mM	0.1525 mL	0.7624 mL	1.5249 mL	3.8122 mL
	20 mM	0.1144 mL	0.5718 mL	1.1437 mL	2.8592 mL
	25 mM	0.0915 mL	0.4575 mL	0.9149 mL	2.2873 mL
	30 mM	0.0762 mL	0.3812 mL	0.7624 mL	1.9061 mL
	40 mM	0.0572 mL	0.2859 mL	0.5718 mL	1.4296 mL
	50 mM	0.0457 mL	0.2287 mL	0.4575 mL	1.1437 mL
	60 mM	0.0381 mL	0.1906 mL	0.3812 mL	0.9531 mL
	80 mM	0.0286 mL	0.1430 mL	0.2859 mL	0.7148 mL
	100 mM	0.0229 mL	0.1144 mL	0.2287 mL	0.5718 mL

I-OMe-Tyrphostin AG 538 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:

I-OMe-Tyrphostin AG 5381094048-77-7I-OMe-AG 538IGF-1RInsulin-like growth factor-1 receptorcytotoxic,nutrient-deprivedpancreaticcancercellstumor,inositollipidInhibitorinhibitorinhibit

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I-OMe-Tyrphostin AG 538 (Synonyms: I-OMe-AG 538)

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Complete Stock Solution Preparation Table

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