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Cat. No.: HY-155594

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LT-540-717

LT-540-717 (compound 32) is a potent FLT3 inhibitor (IC₅₀=0.62 nM) with antiproliferative activity. LT-540-717 also inhibits several acquired FLT3 mutations, FLT3 (ITD, D835V), FLT3 (ITD, F691L), FLT3 (D835Y) and FLT3 (D835V). LT-540-717 has potential to be an anti-AML agent.

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

CAS No.: 2143089-35-2
Formula: C₂₄H₂₄N₈O₂
Molecular Weight:456.50

Storage:

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

Data Sheet (268 KB)

LT-540-717 Chemical Structure

CAS No.: 2143089-35-2

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Use of MCE Products

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

Biological Activity
- Description
- Cellular Effect
Chemical Information
Protocols (2)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
ACHN	GI₅₀	<1 μM Compound: 32; LT-540-717	Antiproliferative activity against human ACHN cells assessed as inhibition of cell growth Antiproliferative activity against human ACHN cells assessed as inhibition of cell growth	[PMID: 37163951]
BaF3	IC₅₀	0.009 μM Compound: 32; LT-540-717	Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/D835V mutant assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/D835V mutant assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 37163951]
BaF3	IC₅₀	0.039 μM Compound: 32; LT-540-717	Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 37163951]
BaF3	IC₅₀	0.043 μM Compound: 32; LT-540-717	Antiproliferative activity against mouse BaF3 cells harboring FLT3 D835V mutant assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against mouse BaF3 cells harboring FLT3 D835V mutant assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 37163951]
BaF3	IC₅₀	0.054 μM Compound: 32; LT-540-717	Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/N676D mutant assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/N676D mutant assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 37163951]
BaF3	IC₅₀	0.095 μM Compound: 32; LT-540-717	Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/F691L mutant assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/F691L mutant assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 37163951]
BaF3	IC₅₀	2.922 μM Compound: 32; LT-540-717	Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 37163951]
HL-60	IC₅₀	972.1 nM Compound: 32; LT-540-717	Antiproliferative activity against human HL-60 cells expressing low level wild type FLT3 assessed as inhibition of cell growth Antiproliferative activity against human HL-60 cells expressing low level wild type FLT3 assessed as inhibition of cell growth	[PMID: 37163951]
K562	IC₅₀	572.1 nM Compound: 32; LT-540-717	Antiproliferative activity against human K562 cells deficit of oncogenic FLT3 assessed as inhibition of cell growth Antiproliferative activity against human K562 cells deficit of oncogenic FLT3 assessed as inhibition of cell growth	[PMID: 37163951]
KM12	GI₅₀	<1 μM Compound: 32; LT-540-717	Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth	[PMID: 37163951]
LOX IMVI	GI₅₀	<1 μM Compound: 32; LT-540-717	Antiproliferative activity against human LOX IMVI cells assessed as inhibition of cell growth Antiproliferative activity against human LOX IMVI cells assessed as inhibition of cell growth	[PMID: 37163951]
MOLM-13	IC₅₀	16.3 nM Compound: 32; LT-540-717	Antiproliferative activity against human MOLM-13 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth Antiproliferative activity against human MOLM-13 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth	[PMID: 37163951]
MV4-11	IC₅₀	0.015 μM Compound: 32; LT-540-717	Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 37163951]
NCI-H460	GI₅₀	<1 μM Compound: 32; LT-540-717	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth	[PMID: 37163951]
PBMC	IC₅₀	831.3 nM Compound: 32; LT-540-717	Cytotoxicity against human PBMC cells assessed as inhibition of cell growth Cytotoxicity against human PBMC cells assessed as inhibition of cell growth	[PMID: 37163951]
SR	GI₅₀	<1 μM Compound: 32; LT-540-717	Antiproliferative activity against human SR cells assessed as inhibition of cell growth Antiproliferative activity against human SR cells assessed as inhibition of cell growth	[PMID: 37163951]
SR	GI₅₀	0.3 μM Compound: 32; LT-540-717	Antiproliferative activity against human SR cells not addicted to FLT3 ITD mutant assessed as inhibition of cell growth Antiproliferative activity against human SR cells not addicted to FLT3 ITD mutant assessed as inhibition of cell growth	[PMID: 37163951]
SW-620	GI₅₀	<1 μM Compound: 32; LT-540-717	Antiproliferative activity against human SW-620 cells assessed as inhibition of cell growth Antiproliferative activity against human SW-620 cells assessed as inhibition of cell growth	[PMID: 37163951]
THP-1	IC₅₀	903.5 nM Compound: 32; LT-540-717	Antiproliferative activity against human THP-1 cells expressing wild type FLT3 assessed as inhibition of cell growth Antiproliferative activity against human THP-1 cells expressing wild type FLT3 assessed as inhibition of cell growth	[PMID: 37163951]
U-937	IC₅₀	692.3 nM Compound: 32; LT-540-717	Antiproliferative activity against human U-937 cells expressing low level wild type FLT3 assessed as inhibition of cell growth Antiproliferative activity against human U-937 cells expressing low level wild type FLT3 assessed as inhibition of cell growth	[PMID: 37163951]

Chemical Information

CAS No. 2143089-35-2
Molecular Weight 456.50
Formula C₂₄H₂₄N₈O₂
SMILES

O=C(NC1=CC=C(N2CCNCC2)C=C1)C3=NNC=C3NC4=NC=NC(OC5=CC=CC=C5)=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.

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]. Zhi Y, et al. Rational design of 4-((6-phenoxypyrimidin-4-yl)amino)-N-(4-(piperazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide (LT-540-717) as orally bioavailable FLT3 inhibitor. Eur J Med Chem. 2023 Aug 5;256:115448. [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.

Bioz

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100 mg

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