JAK3/BTK-IN-6

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JAK3/BTK-IN-6 (compound 14h) is a potent BTK and JAK3 dual inhibitor, with IC₅₀ values of 0.6 and 0.4 nM, respectively. JAK3/BTK-IN-6 shows good metabolic stability in human liver microsome. JAK3/BTK-IN-6 can be used for hematological and immune diseases research.

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

JAK3/BTK-IN-6 Chemical Structure

CAS No. : 2243136-03-8

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JAK1 JAK2 JAK3 Tyk2 JAK

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

JAK3

0.4 nM (IC₅₀)

JAK2

657.9 nM (IC₅₀)

JAK1

>1000 nM (IC₅₀)

Tyk2

>1000 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEL	IC₅₀	1.1 μM Compound: 14h	Antiproliferative activity against human HEL cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HEL cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
JeKo-1	IC₅₀	0.5 μM Compound: 14h	Antiproliferative activity against human JeKo1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human JeKo1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
OCI-Ly10	IC₅₀	1 μM Compound: 14h	Antiproliferative activity against human OCI-LY10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human OCI-LY10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
Raji	IC₅₀	1.7 μM Compound: 14h	Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
Ramos	IC₅₀	0.5 μM Compound: 14h	Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]

In Vitro

JAK3/BTK-IN-6 (compound 14h) shows antiproliferative activities against hematopoietic cells (Raji, Romas, HEL, Jeko-1, and OCI-LY10), with IC₅₀ values of 1.7, 0.5, 1.1, 0.5, and 1-10, respectively^[1].

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

Molecular Weight

455.20

Formula

C₂₁H₁₇BF₃N₅O₃

CAS No.

2243136-03-8

SMILES

C=CC(NC1=CC(NC2=C(C=NC(NC3=CC=C4B(OCC4=C3)O)=N2)C(F)(F)F)=CC=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Ren J, et al. Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. Bioorg Med Chem. 2020 Jan 15;28(2):115236. [Content Brief]

JAK3/BTK-IN-6 Related Classifications

Inflammation/Immunology

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

JAK3/BTK-IN-62243136-03-8BtkJAKBruton tyrosine kinaseJanus kinaseantiproliferativehematopoietic cellRajiRomasHELJeko-1OCI-LY10immune diseasesInhibitorinhibitorinhibit

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