AMG-548

Name: AMG-548
Brand: MedChemExpress
SKU: HY-108642
Rating: 4.5 (1 reviews)

Cat. No.: HY-108642 Purity: 98.28%: FAQs
Data Sheet SDS COA Handling Instructions

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AMG-548, an orally active and selective p38α inhibitor (K_i=0.5 nM), shows slightly selective over p38β (K_i=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC₅₀=3 nM). AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.

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

AMG-548 Chemical Structure

CAS No. : 864249-60-5

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	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 AMG-548:

AMG-548 hydrochloride Get quote
AMG-548 dihydrochloride Get quote

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View All p38 MAPK Isoform Specific Products:

View All Isoforms

p38 MAPK p38α p38β MAPK13 p38δ p38γ

View All Casein Kinase Isoform Specific Products:

View All Isoforms

CK1 CK2

Biological Activity
Purity & Documentation
References
Customer Review

Description

AMG-548, an orally active and selective p38α inhibitor (K_i=0.5 nM), shows slightly selective over p38β (K_i=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC₅₀=3 nM)^[1]. AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε^[2].

IC₅₀ & Target^[1]^[2]

p38α

0.5 nM (Ki)

p38β

3.6 nM (Ki)

p38δ

2600 nM (Ki)

p38γ

4100 nM (Ki)

dog p38α

5.0 nM (Ki)

JNK1

11480 nM (Ki)

JNK2

39 nM (Ki)

JNK3

61 nM (Ki)

CK1

In Vitro

AMG-548 shows >1000 fold selective against p38γ (K_i=2600 nM) and p38δ (k_i=4100 nM). AMG-548 has an modest selectivity against JNK2 (k_i=39 nM) and JNK3 (k_i=61 nM). AMG-548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFa (IC₅₀=3 nM) and IL1b (IC₅₀=7 nM) as well as TNFa induced IL-8 (IC₅₀=0.7 nM) and IL-1b induced IL-6 (IC50₅₀=1.3 nM) in human whole blood^[1].
AMG-548 (10 μM) inhibits the hDvl2 shift^[2].

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

In Vivo

AMG-548 has rat F of 62% and dog F of 47%. The t_1/2 is 4.6 hours in rats and 7.3 hours in dogs^[1].

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

Molecular Weight

461.56

Formula

C₂₉H₂₇N₅O

CAS No.

864249-60-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N(C)C(NC[C@@H](N)CC2=CC=CC=C2)=NC(C3=CC=NC=C3)=C1C4=CC=C5C=CC=CC5=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (216.66 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	2.1666 mL	10.8328 mL	21.6657 mL
5 mM	0.4333 mL	2.1666 mL	4.3331 mL
10 mM	0.2167 mL	1.0833 mL	2.1666 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 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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: ≥99.0% ee.: 100%

Select Batch:

Data Sheet (275 KB) SDS (480 KB)

COA (248 KB)

Handling Instructions (2659 KB)

References

[1]. Lee MR, et al. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alphaprotein. Curr Med Chem. 2005;12(25):2979-94. [Content Brief]

[2]. Verkaar F, et al. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/ɛ. Chem Biol. 2011 Apr 22;18(4):485-94. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1666 mL	10.8328 mL	21.6657 mL	54.1641 mL
	5 mM	0.4333 mL	2.1666 mL	4.3331 mL	10.8328 mL
	10 mM	0.2167 mL	1.0833 mL	2.1666 mL	5.4164 mL
	15 mM	0.1444 mL	0.7222 mL	1.4444 mL	3.6109 mL
	20 mM	0.1083 mL	0.5416 mL	1.0833 mL	2.7082 mL
	25 mM	0.0867 mL	0.4333 mL	0.8666 mL	2.1666 mL
	30 mM	0.0722 mL	0.3611 mL	0.7222 mL	1.8055 mL
	40 mM	0.0542 mL	0.2708 mL	0.5416 mL	1.3541 mL
	50 mM	0.0433 mL	0.2167 mL	0.4333 mL	1.0833 mL
	60 mM	0.0361 mL	0.1805 mL	0.3611 mL	0.9027 mL
	80 mM	0.0271 mL	0.1354 mL	0.2708 mL	0.6771 mL
	100 mM	0.0217 mL	0.1083 mL	0.2167 mL	0.5416 mL

AMG-548 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:

AMG-548864249-60-5AMG548AMG 548p38 MAPKCasein Kinaseselectivep38αp38βTNFαWntdevelopmentstemcellsInhibitorinhibitorinhibit

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AMG-548

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Other Forms of AMG-548:

AMG-548 Related Antibodies

Featured Recommendations

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View All Casein Kinase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

AMG-548 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

AMG-548 Related Classifications

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