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INCB024360 analogue

Cat. No. M2720
INCB024360 analogue Structure
Synonym:

INCB14943

Size Price Availability
5mg USD 70.2  USD78 4-7 Days
10mg USD 97.2  USD108 4-7 Days
50mg USD 277.2  USD308 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 271.64
Formula C9H7ClFN5O2
CAS Number 914471-09-3
Purity >98%
Solubility DMSO >13.6 mg/mL
Storage at -20°C
References

Structural insights into the binding mechanism of IDO1 with hydroxylamidine based inhibitor INCB14943.
Wu Y, et al. Biochem Biophys Res Commun. 2017 May 27;487(2):339-343. PMID: 28412361.

Biological and clinical significance of tryptophan-catabolizing enzymes in cutaneous T-cell lymphomas.
Maliniemi P, et al. Oncoimmunology. 2017 Feb 10;6(3):e1273310. PMID: 28405495.

The rationale of indoleamine 2,3-dioxygenase inhibition for cancer therapy.
Brochez L, et al. Eur J Cancer. 2017 May;76:167-182. PMID: 28324751.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: INCB024360 analogue, INCB14943 supplier, IDO, inhibitors

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