acute myelogenous leukemia

Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.

Pivanex (Pivalyloxymethyl butyrate) is an orally active HDAC inhibitor and an antimetastatic and antiangiogenic agent. Pivanex downregulates the Bcr-Abl protein and enhances apoptosis.

Amsacrine hydrochloride (acridinyl anisidide hydrochloride) is topoisomerase II inhibitor , is used in the treatment of acute myelogenous leukemia.

TL02-59 is a selective inhibitor of Fgr in Src-family kinase (IC50 = 0.03 nM). TL02-59 inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia cell growth.

FLT3-IN-4 (FLT3 inhibitor 9u) is a potent and orally effective Fms-like tyrosine receptor kinase 3 (FLT3; IC50=7 nM) inhibitor ,for treating acute myelogenous leukemia.

Tandutinib (CT53518) (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.

JTE-607 is a cytokine production inhibitor. JTE-607 induces apoptosis accompanied by an increase in p21waf1 cip1 in acute myelogenous leukemia cells.

PROTAC CDK9 degrader 4 is a highly potent CDK9 degrader that targets transcriptional regulation and has potential anticancer activity for the study of acute myelogenous leukemia (AML).

Tandutinib hydrochloride (MLN518 hydrochloride) is a potent, selective FLT3 inhibitor with an IC50 of 0.22 μM and also effectively inhibits c-Kit and PDGFR, with IC50 values of 0.17 μM and 0.20 μM, respectively. This compound is clinically applicable for treating acute myelogenous leukemia (AML) and can cross the blood-brain barrier.

LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. LY2457546 demonstrates potent activity against targets that include VEGFR2 (KDR), PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. In vivo, LY2457546 inhibited VEGF-driven autophosphorylation of lung KDR in the mouse and rat in a dose and concentration dependent manner. LY2457546 was well tolerated and exhibited efficacy in a 13762 syngeneic rat mammary tumor models. Additionally, LY2457546 caused complete regression of well-established tumors in an acute myelogenous leukemia (AML) FLT3-ITD mutant xenograft tumor model. The unique spectrum of target activity, potent in vivo anti-tumor efficacy in a variety of rodent and human solid tumor models, exquisite potency against a clinically relevant model of AML, and non-clinical safety profile justify the advancement of LY2457546 into clinical testing. (source: Invest New D......

PHI-101 is an orally available and selective checkpoint kinase 2 (Chk2) inhibitor for the study of refractory acute myelogenous leukemia (AML) and ovarian cancer.

PDE1-IN-6 (compound 6c) functions as a highly selective PDE1 inhibitor, exhibiting an IC 50 value of 7.5 nM. It notably inhibits proliferation and induces apoptosis in acute myelogenous leukemia cells [1].

Bomedemstat (IMG-7289) is an orally active, irreversible inhibitor of lysine-specific demethylase 1 (LSD1) that exhibits antineoplastic activities in mouse models of myeloproliferative neoplasms (MPNs), and can be used for research on acute myelogenous leukemia (AML) and myelofibrosis (MF) [1].