DYRKs-IN-1 hydrochloride

Name: DYRKs-IN-1 hydrochloride
Brand: MedChemExpress
SKU: HY-128758A
Rating: 4.5 (1 reviews)

Cat. No.: HY-128758A Purity: 99.71%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC₅₀s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity.

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

DYRKs-IN-1 hydrochloride Chemical Structure

CAS No. : 1386980-55-7

Size	Price	Stock	Quantity
5 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 3850	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 6150	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

Other Forms of DYRKs-IN-1 hydrochloride:

DYRKs-IN-1 Get quote

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•Related Screening Libraries:

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View All DYRK Isoform Specific Products:

View All Isoforms

DYRK1 DYRK2 DYRK3 DYRK4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

DYRK1A

5 nM (IC₅₀)

DYRK1B

8 nM (IC₅₀)

In Vitro

DYRKs-IN-1 hydrochloride (compound 30) increases the cellular potency against the human colon tumor cell line SW 620 with an EC₅₀ of 27 nM^[1].
DYRKs-IN-1 hydrochloride (Example 183) is a potent DYRKs inhibitor^[2].

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

Molecular Weight

624.52

Formula

C₃₀H₃₁Cl₂N₇O₄

CAS No.

1386980-55-7

Appearance

Solid

Color

Yellow to brown

SMILES

O=C(C1=CC2=CN=C(N3CC(O4)CCC4C3)N=C2NC1=O)NC5=CC(C(NC(C6=CC=CC=C6)CCN)=O)=CC=C5Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 20.83 mg/mL (33.35 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6012 mL	8.0061 mL	16.0123 mL
5 mM	0.3202 mL	1.6012 mL	3.2025 mL
10 mM	0.1601 mL	0.8006 mL	1.6012 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 (sealed storage, away from moisture). 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: ≥ 2.08 mg/mL (3.33 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.33 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 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: ≥ 2.08 mg/mL (3.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). 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 (20.8 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.71%

Select Batch:

Data Sheet (272 KB) SDS (252 KB)

COA (248 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Anderson K, et al. Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6610-5. [Content Brief]

[2]. Kevin Anderson, et al. Pyrido pyrimidines. US20120184542A1.

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.6012 mL	8.0061 mL	16.0123 mL	40.0307 mL
	5 mM	0.3202 mL	1.6012 mL	3.2025 mL	8.0061 mL
	10 mM	0.1601 mL	0.8006 mL	1.6012 mL	4.0031 mL
	15 mM	0.1067 mL	0.5337 mL	1.0675 mL	2.6687 mL
	20 mM	0.0801 mL	0.4003 mL	0.8006 mL	2.0015 mL
	25 mM	0.0640 mL	0.3202 mL	0.6405 mL	1.6012 mL
	30 mM	0.0534 mL	0.2669 mL	0.5337 mL	1.3344 mL