FLT3/CHK1-IN-2

Cat. No.: HY-162367: Data Sheet Handling Instructions
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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).

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FLT3/CHK1-IN-2 화학구조

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MOQ		Minimum order quantity
50 mg		견적 받기
100 mg		견적 받기
250 mg		견적 받기
Other size		견적 받기

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Chk1 Chk2 BUBR1

Biological Activity
순도&문서
References
고객리뷰

제품 설명

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.

분자량

444.47

화학식

C₁₈H₂₃F₃N₆O₂S

SMILES

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

선적

Room temperature in continental US; may vary elsewhere.

보관

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

순도&문서

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]

FLT3/CHK1-IN-2 Related Classifications

몰농도 계산기
농도 희석 계산기

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

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:

FLT3/CHK1-IN-2FLT3Checkpoint Kinase (Chk)Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3MV4-11 AMLInhibitorinhibitorinhibit

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FLT3/CHK1-IN-2

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