Tpl2 Kinase Inhibitor 1

Name: Tpl2 Kinase Inhibitor 1
Brand: MedChemExpress
SKU: HY-12358
Rating: 4.5 (1 reviews)

Cat. No.: HY-12358 Purity: 99.22%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Tpl2 Kinase Inhibitor 1 is a 3-pyridylmethylamino analog, and is a selective Tpl2 inhibitor (IC₅₀=50 nM). Tpl2 consists of COT kinase and MAP3K8. Tpl2 Kinase Inhibitor 1 plays an important role in the regulation of the inflammatory response and the progression of some cancers.

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

Tpl2 Kinase Inhibitor 1 Chemical Structure

CAS No. : 871307-18-5

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 566	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 566	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 660	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1100	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1760	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

1 Publications Citing Use of MCE Tpl2 Kinase Inhibitor 1

•Phytomedicine. 2024 Jan 8, 155346.

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•Related Screening Libraries:

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View All MAP3K Isoform Specific Products:

View All Isoforms

MAP3K5/ASK1 MAP3K7/TAK1 MAP3K8 ASK2

View All p38 MAPK Isoform Specific Products:

View All Isoforms

p38 MAPK p38α p38β MAPK13 p38δ p38γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

MAP3K8

p38

180 μM (IC₅₀)

MK2

110 μM (IC₅₀)

In Vitro

Tpl2 (Cot/MAP3K8) is a serine/threonine kinase in the MAP3K family that is upstream of MEK in the ERK pathway^[1].
Tpl2 Kinase Inhibitor 1 (compound 2p) also inhibits MK2 and p38, with IC₅₀s of 110 μM and 180 μM, respectively in A431 cells^[1].
Tpl2 Kinase Inhibitor 1 inhibits lipopolysaccharide-induced TNF-a production from primary human monocytes and human whole-blood, with IC₅₀s of 0.7 μM and 8.5 μM, respectively^[1].
Cancer Osaka thyroid (COT) kinase (Tpl2) is an important regulator of pro-inflammatory cytokines in macrophages^[2].

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

Molecular Weight

404.83

Formula

C₂₁H₁₄ClFN₆

CAS No.

871307-18-5

Appearance

Solid

Color

Yellow to green

SMILES

N#CC1=C(NC2=CC=C(F)C(Cl)=C2)C3=CC(NCC4=CC=CN=C4)=NC=C3N=C1

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 (247.02 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	2.4702 mL	12.3509 mL	24.7017 mL
5 mM	0.4940 mL	2.4702 mL	4.9403 mL
10 mM	0.2470 mL	1.2351 mL	2.4702 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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.22%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (249 KB) HNMR (119 KB) RP-HPLC (138 KB)

Handling Instructions (2659 KB)

References

[1]. Gavrin LK, et al. Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5288-92. [Content Brief]

[2]. Glatthar R, et al. Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors. J Med Chem. 2016 Aug 25;59(16):7544-60. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.4702 mL	12.3509 mL	24.7017 mL	61.7543 mL
	5 mM	0.4940 mL	2.4702 mL	4.9403 mL	12.3509 mL
	10 mM	0.2470 mL	1.2351 mL	2.4702 mL	6.1754 mL
	15 mM	0.1647 mL	0.8234 mL	1.6468 mL	4.1170 mL
	20 mM	0.1235 mL	0.6175 mL	1.2351 mL	3.0877 mL
	25 mM	0.0988 mL	0.4940 mL	0.9881 mL	2.4702 mL
	30 mM	0.0823 mL	0.4117 mL	0.8234 mL	2.0585 mL
	40 mM	0.0618 mL	0.3088 mL	0.6175 mL	1.5439 mL
	50 mM	0.0494 mL	0.2470 mL	0.4940 mL	1.2351 mL
	60 mM	0.0412 mL	0.2058 mL	0.4117 mL	1.0292 mL
	80 mM	0.0309 mL	0.1544 mL	0.3088 mL	0.7719 mL
	100 mM	0.0247 mL	0.1235 mL	0.2470 mL	0.6175 mL