JAK2/FLT3-IN-3

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JAK2/FLT3-IN-3 (11r) is a dual FLT3 and JAK2 inhibitor, with IC₅₀ values of 2.01 nM, 0.51 nM and 104.40 nM for JAK2, FLT3 and JAK3, respectively. JAK2/FLT3-IN-3 (11r) induces apoptosis and possesses antitumor activity.

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

JAK2/FLT3-IN-3 Chemical Structure

CAS No. : 3038183-53-5

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Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

JAK2

2.01 nM (IC₅₀)

FLT3

0.51 nM (IC₅₀)

JAK3

104.40 nM (IC₅₀)

In Vitro

JAK2/FLT3-IN-3 (11r) exerts potent antiproliferative activity against HEL (IC₅₀ = 1.1 μM), MV4-11 (IC₅₀ = 9.43 nM), RPMI-8226 (IC₅₀ = 0.793 μM), NCI-H929 (IC₅₀ = 0.743 μM), Ba/F3-FLT3-ITD-D835Y (IC₅₀ = 0.099 μM), and Ba/F3-FLT3-ITD-F691L (IC₅₀ = 0.042 μM) cell lines^[1].

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

In Vivo

JAK2/FLT3-IN-3 (11r) shows moderate absorption (T_max = 5.33 h), with a peak concentration of 38.7 ng/mL and an AUC of 522 ng h/mL in rats, and an oral bioavailability of 25.2%^[1].

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

Molecular Weight

611.78

Formula

C₃₄H₄₅N₉O₂

CAS No.

3038183-53-5

SMILES

O=C(NC1=CC=C(C(C)=O)C=C1)N(CC2)CCN2C3=NC(NC4=CC=C(N5CCC(N6CCN(C)CC6)CC5)C=C4)=NC=C3C

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]. Sicong Xu, et al. 2-Aminopyrimidine derivatives as selective dual inhibitors of JAK2 and FLT3 for the treatment of acute myeloid leukemia. Bioorg Chem. 2023 May:134:106442. [Content Brief]

JAK2/FLT3-IN-3 Related Classifications

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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:

JAK2/FLT3-IN-33038183-53-5FLT3JAKApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Janus kinaseHELMV4-11RPMI-8226NCI-H929JAK2Inhibitorinhibitorinhibit

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