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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.

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CAS No.: 1802909-50-7
Formule: C₂₅H₃₅F₃N₂O₅
Masse moléculaire:500.55

Stockage:

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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Use of MCE Products

Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Pureté et documentation
Références
Calculators
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Activité biologique

Description

IC₅₀ & Target^[1]

LSD1

Voir tous les produits spécifiques à Isoform Histone Demethylase :

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.

Essai clinique

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

Chemical Information

CAS No. 1802909-50-7
Masse moléculaire 500.55
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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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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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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Pureté et documentation
Références

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INCB059872 TFA

Voir tous les produits spécifiques à Isoform Histone Demethylase

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

INCB059872 TFA Related Classifications

HY-141677C Related Classifications