PF-05381941

Name: PF-05381941
Brand: MedChemExpress
SKU: HY-120823
Rating: 4.5 (1 reviews)

Cat. No.: HY-120823 Purity: 99.73%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC₅₀s of 156 and186 nM, respectively.

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

PF-05381941 Chemical Structure

CAS No. : 1474022-02-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 297	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 297	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 430	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 860	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1380	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2200	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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MAP3K7/TAK1 MAP3K8 ASK2 MAP3K5/ASK1

View All p38 MAPK Isoform Specific Products:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

PF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC₅₀s of 156 and186 nM, respectively^[1].

IC₅₀ & Target^[1]

p38α

186 nM (IC₅₀)

TAK1

156 nM (IC₅₀)

In Vitro

PF-05381941 inhibits LPS-stimulated release of TNF-αfrom human peripheralmononuclear (PMN) cells with an IC₅₀ of 8 nM^[1].

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

Molecular Weight

466.53

Formula

C₂₇H₂₆N₆O₂

CAS No.

1474022-02-0

Appearance

Solid

Color

Off-white to brown

SMILES

O=C(NC1=CC=C(OC2=CC=NC=C2)C(C)=C1)NC3=CC(C(C)(C)C)=NN3C4=CC=CC(C#N)=C4

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 (214.35 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	2.1435 mL	10.7174 mL	21.4348 mL
5 mM	0.4287 mL	2.1435 mL	4.2870 mL
10 mM	0.2143 mL	1.0717 mL	2.1435 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 (5.36 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.39 mg/mL (2.98 mM); Clear solution

This protocol yields a clear solution of ≥ 1.39 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.9 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: 99.73%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (250 KB) RP-HPLC (218 KB)

Handling Instructions (2659 KB)

References

[1]. Kilty I, et al. TAK1 inhibition in the DFG-out conformation. Chem Biol Drug Des. 2013;82(5):500-505. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1435 mL	10.7174 mL	21.4348 mL	53.5871 mL
	5 mM	0.4287 mL	2.1435 mL	4.2870 mL	10.7174 mL
	10 mM	0.2143 mL	1.0717 mL	2.1435 mL	5.3587 mL
	15 mM	0.1429 mL	0.7145 mL	1.4290 mL	3.5725 mL
	20 mM	0.1072 mL	0.5359 mL	1.0717 mL	2.6794 mL
	25 mM	0.0857 mL	0.4287 mL	0.8574 mL	2.1435 mL
	30 mM	0.0714 mL	0.3572 mL	0.7145 mL	1.7862 mL
	40 mM	0.0536 mL	0.2679 mL	0.5359 mL	1.3397 mL
	50 mM	0.0429 mL	0.2143 mL	0.4287 mL	1.0717 mL
	60 mM	0.0357 mL	0.1786 mL	0.3572 mL	0.8931 mL
	80 mM	0.0268 mL	0.1340 mL	0.2679 mL	0.6698 mL
	100 mM	0.0214 mL	0.1072 mL	0.2143 mL	0.5359 mL

PF-05381941 Related Classifications

Inflammation/Immunology

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:

PF-053819411474022-02-0PF05381941PF 05381941MAP3Kp38 MAPKMAP kinase kinase kinase, MEKK, MAPKKKinflammatorykinaseTNFLPSperipheralmononuclearcellsInhibitorinhibitorinhibit

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PF-05381941

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PF-05381941 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All MAP3K Isoform Specific Products:

View All p38 MAPK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

PF-05381941 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

PF-05381941 Related Classifications

Keywords:

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