myelogenous

Tallimustine HCl is a DNA inhibitor, an AT-specific alkylated antitumor derivative of diamycin.Tallimustine HCl can be used in severe combined immunodeficiency mouse models of adult myelogenous leukemia, which can be used for the treatment of leukemia.

AN-019 (NRC-019) is a Bcr-Abl kinase inhibitor with antitumor activity for the study of chronic myelogenous leukemia (CML) and breast cancer.

Carboxyamidotriazole Orotate (L-651582 Orotate) is a cytostatic inhibitor of non-voltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor that in vitro has been shown to possess antileukaemic activities. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory, and antiangiogenic effects.

K-252c is a staurosporine analog isolated from Nocardiopsis sp. and is a cell-permeable PKC inhibitor (IC50: 2.45 μM). K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase. K-252c causes apoptosis in human chronic myelogenous leukemia cancer cells.

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.

Anticancer Agent 110 exhibits potent in vitro anti-leukemia activity, demonstrating high cytotoxicity against K-562 lineage chronic myelogenous leukemia cells at nanomolar concentrations. It induces DNA damage and subsequently triggers apoptosis [1].

Enocitabine is a nucleoside analog. Enocitabine inhibits the replication of human cytomegalovirus(HCMV) and it also has antileukemic and antiviral activities. Enocitabine is also a potent DNA replication inhibitor and a DNA chain terminator.

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......

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.

Nilotinib N-oxide is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia.

Ranimustine (MCNU) can be used for polycythemia vera and chronic myelogenous leukemia research, which is a nitrosourea alkylating agent [1] [3] [4].

BVB-808 is a selective Jak2 type 1 inhibitor. Janus kinases are critical components of signaling pathways that regulate hematopoiesis. Mutations of the non-receptor tyrosine kinase JAK2 are found in many BCR-ABL-negative myeloproliferative neoplasms. Preclinical results support that JAK2 inhibitors could show efficacy in treating chronic myeloproliferative neoplasms. JAK2 has also been postulated to play a role in BCR-ABL signal transduction. Therefore, inhibitors of JAK2 kinases are turning into therapeutic strategies for treatment of chronic myelogenous leukemia (CML).

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

β-D-Ribofuranose 1,2,3,4-tetraacetate is a precursor in the synthesis of nucleosides with antiproliferative activity against cancer cells.1,2 1.Furukawa, Y., and Honjo, M.A novel method for the synthesis of purine nucleosides using Friedel-Crafts catalystsChem. Pharm. Bull. (Tokyo)16(6)1076-1080(1968) 2.Wicke, L., Engels, J.W., Gambari, R., et al.Synthesis and antiproliferative activity of quinolone nucleosides against the human myelogenous leukemia k-562 cell lineArch. Pharm. (Weinheim)346(10)757-765(2013)

Nilotinib hydrochloride(AMN-107 HCl) is an orally available Bcr-Abl tyrosine kinase inhibitor with antitumor activity for modulation of neuroinflammation and cognitive deficits, and may be used in studies of chronic myelogenous leukemia.

BCR-ABL-IN-7 is a WT and T315I mutant ABL kinase inhibitor.BCR-ABL-IN-7 potently inhibits WT and T315I mutant ABL kinase activity.BCR-ABL-IN-7 can be used in chronic myelogenous leukemia (CML) research.

Nilotinib hydrochloride dihydrate is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia.

PD180970 is an inhibitor of Bcr-Abl with IC50s of 5 nM, 0.8 nM and 50 nM for the autophosphorylation of p210Bcr-Abl, Src and Kit. PD180970 can be used in studies about chronic 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.

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.

Gypsogenin (639-14-5) is a naturally occurring biochemical that shows anti-ABL1 kinase and anti-chronic Myelogenous Leukemia activities.

XX-650-23 is a small molecule CREB inhibitor that blocks the critical interaction between CREB and its required coactivator, CBP (CREB-binding protein), inducing apoptosis and cell cycle arrest in AML cells, and can be used in the study of acute myelogenous leukaemia (AML).

GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively.

Zosuquidar (LY335979) is an inhibitor of P-glycoprotein with a Ki value of 59 nM. Zosuquidar has anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research.

Imatinib is a multi-target inhibitor of v-Abl, c-Kit, and PDGFR (IC50: 0.6 μM, 0.1 μM, and 0.1 μM, respectively). Imatinib is used to treat chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs), and a number of other malignancies.

Nilotinib dihydrochloride dihydrate is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia.

Eupahualin C shows significant activities against cell lines of human chronic myelogenous leukemia (K562) and human bone cancer (U2OS).

Tandutinib hydrochloride (MLN518 hydrochloride) is a potent, selective FLT3 inhibitor with an IC50 of 0.22 μM. It 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 possesses the capability to cross the blood-brain barrier.

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

GNF-5 is a specific non-ATP competitive inhibitor of Bcr-Abl (IC50: 0.22±0.1 uM, Wild-type Abl). It is an analog of GNF-2 with improved pharmacokinetic properties.

ODN 1585 is a potent inducer of IFN and TNFα production, a potent stimulator of NK (natural killer) and can be used as a vaccine adjuvant.ODN 1585 enhances the function of CD8+ T cells, including CD8+ T cell-mediated IFN-γ production.ODN 1585 induces regression of established melanomas in mice and has been shown to inhibit malaria in mice. ODN 1585 can be used to study acute myelogenous leukaemia (AML) and malaria.

Tyrphostin AG957, a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity restores beta1 integrin-mediated adhesion and inhibitory signaling in chronic myelogenous leukemia hematopoietic progenitors[1].

Adaphostin (NSC-680410) is a p210Bcr/Abl tyrosine kinase inhibitor with IC50 of 14 μM.

BCR-ABL-IN-1 is a BCR-ABL tyrosine kinase inhibitor (pIC50: 6.46) and may be used in the research of chronic myelogenous leukemia.

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

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.