TAK1/MAP4K2 inhibitor 1

Name: TAK1/MAP4K2 inhibitor 1
Brand: MedChemExpress
SKU: HY-77251
Rating: 4.5 (1 reviews)

Cat. No.: HY-77251 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC₅₀s of 41.1 nM and 18.2 nM, respectively.

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

TAK1/MAP4K2 inhibitor 1 Chemical Structure

CAS No. : 1315330-11-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 450	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 450	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 148	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 370	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 475	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1280	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE TAK1/MAP4K2 inhibitor 1

•Korean J Physiol Pharmacol. 2022 Nov 1;26(6):469-478. [Abstract]

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MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

View All MAP3K Isoform Specific Products:

View All Isoforms

MAP3K7/TAK1 MAP3K8 ASK2 MAP3K5/ASK1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

TAK1

41.1 nM (IC₅₀)

MAP4K2

18.2 nM (IC₅₀)

In Vivo

TAK1/MAP4K2 inhibitor 1 has moderate terminal elimination half-life (t_1/2=2.94 h for mice (1 mg/kg, iv))^[1].

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

Molecular Weight

552.59

Formula

C₂₉H₃₁F₃N₆O₂

CAS No.

1315330-11-0

Appearance

Solid

Color

White to light yellow

SMILES

CC(N1)=CC2=C1N=CN=C2OC3=C(C)C=CC(C(NC4=CC=C(CN5CCN(CC)CC5)C(C(F)(F)F)=C4)=O)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (90.48 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	1.8097 mL	9.0483 mL	18.0966 mL
5 mM	0.3619 mL	1.8097 mL	3.6193 mL
10 mM	0.1810 mL	0.9048 mL	1.8097 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 2.75 mg/mL (4.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (4.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: 99.90%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (257 KB) HNMR (290 KB) RP-HPLC (255 KB) LCMS (330 KB)

Handling Instructions (2659 KB)

References

[1]. Tan L, et al. Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J Med Chem. 2015 Jan 8;58(1):183-96. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8097 mL	9.0483 mL	18.0966 mL	45.2415 mL
	5 mM	0.3619 mL	1.8097 mL	3.6193 mL	9.0483 mL
	10 mM	0.1810 mL	0.9048 mL	1.8097 mL	4.5241 mL
	15 mM	0.1206 mL	0.6032 mL	1.2064 mL	3.0161 mL
	20 mM	0.0905 mL	0.4524 mL	0.9048 mL	2.2621 mL
	25 mM	0.0724 mL	0.3619 mL	0.7239 mL	1.8097 mL
	30 mM	0.0603 mL	0.3016 mL	0.6032 mL	1.5080 mL
	40 mM	0.0452 mL	0.2262 mL	0.4524 mL	1.1310 mL
	50 mM	0.0362 mL	0.1810 mL	0.3619 mL	0.9048 mL
	60 mM	0.0302 mL	0.1508 mL	0.3016 mL	0.7540 mL
	80 mM	0.0226 mL	0.1131 mL	0.2262 mL	0.5655 mL