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Cat. No.: HY-141677C

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INCB059872 TFA

INCB059872 TFA is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor that achieves inhibitory activity through the formation of covalent FAD-adducts. INCB059872 TFA can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 TFA can be used for the research of myeloid leukemia.

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

CAS No.: 1802909-50-7
Formula: C₂₅H₃₅F₃N₂O₅
Molecular Weight:500.55

Storage:

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

INCB059872 TFA Chemical Structure

CAS No.: 1802909-50-7

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

LSD1

All Histone Demethylase Isoforms :

In Vitro

INCB059872 TFA can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b^[1].

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

Western Blot Analysis^[1]

Cell Line:

293T cells
Concentration:

250 nM
Incubation Time:

48 hours
Result:

Increased enhancer activity and gene expression.

In Vivo

INCB059872 (p.o.) TFA can significantly prolong the median survival time of mice with MLL-AF9-expressing leukemia, induce the differentiation of primitive leukemic cells in mice, reduce the formation of primitive cell colonies, and restore hematological clinical indicators to the levels observed in normal non-leukemic mice^[1].

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

Animal Model:

Mice^[1]
Dosage:

10 mg/kg
Administration:

P.o.; 0, 4, or 6 days
Result:

Single-cell RNA-seq revealed changes in bone marrow progenitor populations.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1802909-50-7
Molecular Weight 500.55
Formula C₂₅H₃₅F₃N₂O₅
SMILES

OC(C(F)(F)F)=O.OC(C1(CCC1)CN2CCC(COC)(CC2)CN[C@H]3[C@H](C4=CC=CC=C4)C3)=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]. Lee S H, et al. Discovery of INCB059872, a novel FAD-directed LSD1 inhibitor that is effective in preclinical models of human and murine AML[J]. Cancer Research, 2016, 76(14_Supplement): 4712-4712.

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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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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Purity & Documentation
References

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INCB059872 TFA

All Histone Demethylase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

INCB059872 TFA Related Classifications

HY-141677C Related Classifications