Free shipping on all orders over $ 500

INCB024360 analogue

Cat. No. M2720
INCB024360 analogue Structure
Synonym:

INCB14943

Size Price Availability Quantity
10mg USD 55  USD55 In stock
50mg USD 165  USD165 In stock
100mg USD 275  USD275 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

INCB024360 is a potent IDO1 inhibitor (IC50 value of 10 nM) with desirable pharmaceutical properties, is poised to start clinical trials in cancer patients. In cellular assays, INCB024360 selectively inhibits human IDO1 with IC(50) values of approximately 10nM, demonstrating little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).

In vivo: In mice bearing GM-CSF-secreting B16 tumors, INCB024360 (75 mg/kg b.i.d) causes dose dependent inhibition of tumor growth. INCB024360 significantly suppresses tumor growth in immunocompetent, but not immunodeficient, mice.

In vitro: In HeLa cells, INCB024360 shows higher inhibitory activity on IDO1 with IC50 of 19 nM. In coculture systems of human allogeneic lymphocytes with dendritic cells or tumor cells, INCB024360, via IDO1 inhibition, reverses T-cell suppression mediated by IDO-expressing HeLa cells or DCs, and increases the proliferation and functional activity of CD4+ T cells, CD8+ T cells, and NK cells.

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Mice bearing GM-CSF-secreting B16 tumors
Formulation 5% DMA, 47.5% propylene glycol
Dosages 75 mg/kg b.i.d
Administration s.c.
Chemical Information
Molecular Weight 271.64
Formula C9H7ClFN5O2
CAS Number 914471-09-3
Solubility (25°C) DMSO >13.6 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Wu Y, et al. Biochem Biophys Res Commun. Structural insights into the binding mechanism of IDO1 with hydroxylamidine based inhibitor INCB14943.

[2] Maliniemi P, et al. Oncoimmunology. Biological and clinical significance of tryptophan-catabolizing enzymes in cutaneous T-cell lymphomas.

[3] Brochez L, et al. Eur J Cancer. The rationale of indoleamine 2,3-dioxygenase inhibition for cancer therapy.

Related IDO Products
IDO-IN-18

IDO-IN-18 is an IDO inhibitor.

IDO1-IN-21

IDO1-IN-21 is an IDO1 inhibitor (IC50 = 0.64 μM).

IDO1-IN-22

IDO1-IN-22 is a IDO1 inhibitor (biochemical hIDO1 IC50: 67.4 nM, HeLa hIDO1 IC50: 17.6 nM).

IDO1/TDO-IN-6

IDO1/TDO-IN-6 is a dual inhibitor of IDO1/TDO with IC50s of 2.25 and 2.89 μM, respectively.

IDO-IN-13 

IDO-IN-13 is a potent indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an EC50 of 17 nM, extracted from patent WO2019040102A1, example 43.

  Catalog
Abmole Inhibitor Catalog




Keywords: INCB024360 analogue, INCB14943 supplier, IDO, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.