antileukemic activity

Gilteritinib (ASP2215) is a potent inhibitor of FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preclinical studies, gilteritinib demonstrated strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 clinical trials for acute myeloid leukemia.

Anticancer agent 110 is an anticancer compound with cytotoxic, antitumor, and antileukemic activity that triggers DNA damage and apoptosis and is used in the study of chronic granulocytic leukemia.

Hepsulfam is an anticancer agent. It also displays excellent antileukemic activity (a median IC50: 0.91 μg mL in a panel of different tumors).

PD166326, a pyridopyrimidine-type inhibitor of receptor tyrosine kinases, demonstrates antileukemic activity with IC50 values of 6 nM for Src and 8 nM for Abl. [1] [2].

KPT-251 is a selective nuclear export inhibitor.

Moflomycin is an anthracycline derivative. It exhibits a higher antileukemic activity compared to other anthracyclines.

Botryodiplodin, an antibiotic, has antileukemic activity from Botryodiplodia theobromae. It has the property of turning the skin of the individual in various shades of pink 2-3 hrs after application. It is a toxic metabolite of Penicillium carneo-lutescen

Hisphen shows antileukemic activity.

Itacnosertib (TP-0184) is an orally available ACRV1 (ALK-2), FLT3 and JAK2 inhibitor that inhibits the growth of tumor cells overexpressing ALK-2, overcomes FLT3 inhibitor resistance and synergistically inhibits AML growth with venetoclax, and possesses potential antitumor and antileukemic activity.

1. Triptonide (PG 492) is effective in the treatment of autoimmune diseases and has potent antileukemic and antitumor activities. 2. Triptonide possesses anti-inflammatory activity, upregulate the expression of IL-37, and this expression was suppressed by ERK1 2 and p38 MAPK inhibitors.

S-(N-PhenethylthiocarbaMoyl)-L-cysteine (PEITC-Cys) is an anticarcinogenic agent that exhibits antileukemic activity by inhibiting DNA synthesis in HL60 cells [1] and acts as an inhibitor of P450 [2].

AZD-1897 is a highly efficient ATP-competitive pan-PIM inhibitor with anticancer and antileukemic activity, inhibiting PIM1, PIM2, and PIM3, which can be used to study multiple myeloma.

HDAC-IN-49 is a potent, non-selective inhibitor of HDAC (HDAC), demonstrating IC50 values of 13 nM for HDAC1, 14 nM for HDAC2, 21 nM for HDAC3, 1880 nM for HDAC4, and 10 nM for HDAC6. This compound exhibits significant antileukemic activity while maintaining low cytotoxicity towards healthy cells.

(+)SHIN2, an isomer of (-)SHIN2, is an inhibitor of serine hydroxymethyltransferase (SHMT) with antileukemic effects and shows synergistic activity with Methotrexate in in vivo xenotransplantation models [1].

Caspase-3 activator 3 (compound 2h) effectively induces apoptosis in HL-60 and K562 cells by substantially activating caspase-3, demonstrating antileukemic activity with IC50 values of 42.89 μM and 33.61 μM, respectively [1].

IMGN-779 (Anti-CD33 Antibody) is a humanized antibody targeting CD33 with antileukemic activity, which can be used to study leukemia.

Microhelenin C has significant antileukemic activity.

Bruceantinoside A has antileukemic activity.

Dehydrobruceantinol shows bitter taste and has antileukemic activity.

Eucannabinolide exhibits in vivo antileukemic activity.

(+)-Nortrachelogenin is a lignan isolated from Wikstroemia indica C.A. Meyer (Thymelaeaceae). (+)-Nortrachelogenin possesses antileukemic activity.

Tagitinin F possesses antileukemic activity; it also shows in vitro leishmanicidal activities against Leishmania braziliensis promastigotes and amastigotes.