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Cat. No.: HY-162367

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FLT3/CHK1-IN-2

FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and CHK1, with IC₅₀s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML).

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

Formula: C₁₈H₂₃F₃N₆O₂S
Molecular Weight:444.47

Storage:

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

Data Sheet (268 KB)

FLT3/CHK1-IN-2 Chemical Structure

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Checkpoint Kinase (Chk) Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	26.37 nM Compound: 30	Antiproliferative activity against mouse BaF3 cells expressing FLT3 D835V mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader Antiproliferative activity against mouse BaF3 cells expressing FLT3 D835V mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader	[PMID: 38389894]
BaF3	IC₅₀	28.96 nM Compound: 30	Antiproliferative activity against mouse BaF3 cells expressing FLT3 F691L mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader Antiproliferative activity against mouse BaF3 cells expressing FLT3 F691L mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader	[PMID: 38389894]
BaF3	IC₅₀	29.3 nM Compound: 30	Antiproliferative activity against mouse BaF3 cells expressing FLT3 D835F mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader Antiproliferative activity against mouse BaF3 cells expressing FLT3 D835F mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader	[PMID: 38389894]
BaF3	IC₅₀	30.24 nM Compound: 30	Antiproliferative activity against mouse BaF3 cells expressing FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader Antiproliferative activity against mouse BaF3 cells expressing FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader	[PMID: 38389894]
BaF3	IC₅₀	75.81 nM Compound: 30	Antiproliferative activity against mouse BaF3 cells expressing FLT3 ITD D835Y mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader Antiproliferative activity against mouse BaF3 cells expressing FLT3 ITD D835Y mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader	[PMID: 38389894]
MV4-11	IC₅₀	2.96 nM Compound: 30	Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD/TKD mutant incubated for 72 hrs by absorbance based microplate reader Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD/TKD mutant incubated for 72 hrs by absorbance based microplate reader	[PMID: 38389894]

In Vitro

FLT3/CHK1-IN-2 shows antiproliferation activity against MV4-11 cell (IC₅₀: <4 nM)^[1].
FLT3/CHK1-IN-2 shows antiproliferative activity against BaF3 cells with a variety of FLT3 mutations (IC₅₀: 28.96, 29.30, 26.37, 30.24, 75.81 nM for BaF3-FLT3-F691L, BaF3-FLT3-D835F, BaF3-FLT3-D835V, BaF3-FLT3-ITD, BaF3-FLT3-ITD/D835Y cells)^[1].
FLT3/CHK1-IN-2 (0-100 nM) inhibits the phosphorylation of FLT3 and its main downstream effectors, STAT5 (Tyr694), AKT (Ser473) and ERK (Tyr204) in MV4-11 cells, and decreases the pS296-CHK1 level and the c-Myc protein expression level^[1].

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

In Vivo

FLT3/CHK1-IN-2 (20 mg/kg, p.o.) has favorable PK properties, with the C_max of 2213.07 ng/mL, and the AUC(0−t) of 2736.58 h·ng/mL^[1].

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

Chemical Information

Molecular Weight 444.47
Formula C₁₈H₂₃F₃N₆O₂S
SMILES

NCCCNC1=NC(NC2=CC(CCN(S(=O)(C)=O)C3)=C3C=C2)=NC=C1C(F)(F)F
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Deng M, et al. Discovery of 5-trifluoromethyl-2-aminopyrimidine derivatives as potent dual inhibitors of FLT3 and CHK1. RSC Med Chem. 2023 Dec 7;15(2):539-552. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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FLT3/CHK1-IN-2

All Checkpoint Kinase (Chk) Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

FLT3/CHK1-IN-2 Related Classifications

HY-162367 Related Classifications