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IACS-010759

Chemical Structure IACS-010759

CAS No.: 1570496-34-2

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IACS-010759(IACS010759)

Catalog No.: GY05498Research Only, Not for Human Use!

IACS-010759 (IACS010759) is a small molecule inhibitor of mitochondrial oxidative phosphorylation (OXPHOS), targets complex I of the mitochondrial electron transport chain

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Purity & Documentation Purity: > 98%(HPLC) Select Batch:

Biological Activity

IACS-010759 (IACS010759) is a small molecule inhibitor of mitochondrial oxidative phosphorylation (OXPHOS), targets complex I of the mitochondrial electron transport chain; decreases cell viability and increases apoptosis with EC50 values between 1 nM-50 nM across multiple lines; robustly inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS, reduces aspartate production that leads to impaired nucleotide biosynthesis; potently inhibits tumor growth of brain cancer and AML in vivo.

Physicochemical Properties

M.Wt 562.568
Formula C25H25F3N6O4S
CAS No. 1570496-34-2
Storage
Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 3 Month
Shipping
Solubility

Chemical Name 5-(5-methyl-1-(3-(4-(methylsulfonyl)piperidin-1-yl)benzyl)-1H-1,2,4-triazol-3-yl)-3-(4-(trifluoromethoxy)phenyl)-1,2,4-oxadiazole

Clinical Information

Blood Cancer
Phase 1 Clinical

References

1. Molina JR, et al. Nat Med. 2018 Jun 11. doi: 10.1038/s41591-018-0052-4.

2. Vangapandu HV, et al. Oncotarget. 2018 May 18;9(38):24980-24991.

3. Lissanu Deribe Y, et al. Nat Med. 2018 Jun 8. doi: 10.1038/s41591-018-0019-5.

4. Jennifer Molina, et al. Abstract 4971: IACS-010759, a novel inhibitor of complex I in Phase I clinical development to target OXPHOS dependent tumors. AACR. DOI: 10.1158/1538-7445.

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