chronic myelogenous leukemia

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

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

Nilotinib (AMN107) is a Bcr-Abl tyrosine kinase inhibitor with oral activity. Nilotinib has antitumor activity and may be used for the treatment of Imatinib-resistant chronic myelogenous leukemia (CML).

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

iHCK-37 (ASN05260065) is a selective Hck inhibitor with antitumor activity, blocking HIV-1 viral replication. iHCK-37 reduces PI3K/AKT and MAPK/ERK pathway activation after erythropoietin induction in high Hck-expressing cells, useful in chronic myelogenous leukemia (CML) research.

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.

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.

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.

MMP-2Inhibitor-4 (Compound 5g) is an MMP-2 inhibitor with an IC50 of 152.62 nM. It effectively reduces MMP-2 levels in K562 cell lines by stably binding to the active site of MMP-2 and exhibits strong anti-angiogenic effects in ACHN cell lines. MMP-2Inhibitor-4 shows potential for research in chronic myelogenous leukemia (CML).

BCR-ABL-IN-11 (Compound 2) is an inhibitor of BCR-ABL, exhibiting anticancer activity against chronic myelogenous leukemia (CML) with an IC50 value of 129.61 μM in K562 cells.

Reveromycin C is a polyketide compound originally isolated from Streptomyces, exhibiting antifungal activity against Candida albicans with a MIC of 2.0 μg/mL at pH 3 and >500 μg/mL at pH 7.4. It inhibits EGF-induced mitogenic activity in Balb/MK mouse epidermal cell lines. Additionally, it reverses the morphology of sarcoma virus-transformed NRK rat kidney cells (EC50 = 1.58 μg/mL) and inhibits the proliferation of KB cells and K562 human chronic myelogenous leukemia cells (IC50 = 2.0 μg/mL for both).

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].

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.

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.

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.

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

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

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

IST5-002 (N6-Benzyladenosine-5'-phosphate) is a selective Stat5a/b inhibitor with anticancer activity that inhibits the transcriptional activity of Stat5a/b and induces apoptosis and death of prostate cancer cells and chronic myelogenous leukemia (CML) cells, which can be used for cancer research.

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

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

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

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).

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.