imatinib-resistant

AKI603 is a novel small molecule inhibitor of Aurora kinase A (AurA)(IC50 = 12.3 nM). AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells[1][2].

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).

Anticanceragent 259 (Compound 3g) is a telmisartan-based cell death regulator that disrupts the STAT5 signaling pathway, thereby increasing the sensitivity of resistant cells to imatinib, with an SC50 of 1.5 μM.

Ki11502 is a multi-target receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGFβ/α receptors (with an IC50 of less than 10 nM). It specifically suppresses PDGFβ receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Additionally, Ki11502 induces apoptosis and exhibits significant antiproliferative effects against specific leukemia subgroups, including those with Imatinib-resistant mutations. It is particularly suitable for studying the role of PDGF in vascular diseases and the involvement of proteoglycans in atherosclerosis.

AK-HW-90 (compound 2B) is a potent pan-Bcr-Abl inhibitor that shows significant inhibitory activity against Imatinib-resistant mutants. It inhibits the resistant Bcr-AblT315I mutant with an IC50 of 0.65 nM. AK-HW-90 offers potential anti-cancer properties and can be utilized in chronic myeloid leukemia (CML) research.

BLU-654 is an orally active antitumor agent and KIT inhibitor. It targets wild-type KIT, PDGFRβ, and serves as a highly selective inhibitor of KITV654A among most other kinases in the kinome. BLU-654 demonstrates sustained antitumor activity in xenograft mouse models derived from KITV654A cells. It is applicable for research related to Imatinib-resistant gastrointestinal stromal tumors.

MPT0B002 is a microtubule inhibitor that acts by downregulating T315I mutant Bcr-Abl and inducing apoptosis of imatinib-resistant chronic myeloid leukemia cells.

HS-438 inhibits imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia.

PPARγ agonist 3, also known as Compound 18a, is a potent and selective agonist of PPARγ. This compound does not exhibit cytotoxicity towards both non-resistant and resistant cells. Notably, PPARγ agonist 3 demonstrates antitumor efficacy exclusively when co-administered with Imatinib [1].

PPARγ agonist 4 (Compound 18b), a potent and selective PPARγ agonist, demonstrates antitumor efficacy only when used in conjunction with Imatinib and does not exhibit cytotoxic effects on either non-resistant or resistant cells [1].

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

AP23464 represents a highly specialized ATP-based small molecule tyrosine kinase inhibitor specifically engineered to target the catalytic domain of Abl and Src kinases along with the Kit receptor with exceptional inhibitory potency and selectivity, effectively facilitating the measurable blockade of phosphorylation-mediated signaling across various preclinical experimental models to evaluate the suppression of oncogenic driver activities during strictly monitored laboratory observation periods and biochemical investigations to ensure high experimental sensitivity.

ON012380 is a non-ATP-competitive Bcr-Abl inhibitor, potently inhibiting imatinib-resistant Bcr-Abl mutants such as T315I.

PHA-680626 is a potent and selective PLK inhibitor. PHA-680626 exhibits anti-proliferative and pro-apoptotic activity on Imatinib-resistant chronic myeloid leukemia cell lines and primary CD34+ cells by inhibition of both Bcr-Abl tyrosine kinase and Aurora kinases. PHA-680626 inhibits Plk1 (IC50 = 0.53 μM), Plk2 (IC50 = 0.07 μM) and Plk3 (IC50 = 1.61 μM).

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.

ON044580 is an effective non-ATP-competitive inhibitor of JAK2, characterized as an α-benzoylstyrylbenzyl thioether. It exhibits IC50 values of 1.23 μM for wild type JAK2 and 1.09 μM for the V617F mutation. The compound inhibits JAK2 kinase activity by binding to the STAT-5 binding domain or the allosteric site of JAK2. In JAK2V617F-positive leukemia cells, ON044580 suppresses proliferation and induces apoptosis in Imatinib-resistant chronic myeloid leukemia (CML) cells. It also inhibits both wild type and T315I mutant forms of the BCR-ABL kinase. ON044580 is used in research for myeloproliferative diseases characterized by abnormal JAK/STAT signaling.

Nilotinib (Standard) is a reference standard for research and analysis in studies involving Nilotinib. 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).

Ladanein is a phytochemicals inhibitor that is known to disrupt the interactions of core and other hepatitis C virus (HCV) proteins.Ladanein possesses free radicals DPPH and ABTS +.scavenging activity, it also displays moderate (20-40 microM) activities against K562, K562R (imatinib-resistant), and 697 human leukemia cell lines.