aml cell lines

IDH2R140Q-IN-2 is an orally active and potent IDH2R140Q inhibitor with an IC50 of 29 nM.IDH2R140Q-IN-2 possesses potential antitumour activity, reducing D2HG production in TF-1 cell lines carrying the IDH2R140Q mutation (IC50 of 10 nM) and inhibiting tumour tissue D2HG levels.IDH2R140Q-IN-2 is suitable for the study of acute myeloid leukaemia (AML).

TPC-144 is a potent and selective LSD1 inhibitor with a reversible inhibition mechanism. TPC-144 has antitumor activity in several human AML and SCLC cell lines and xenograft models.

Sorafenib N-oxide is an active metabolite of sorafenib , an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases. Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD; Kd = 70 nM) and inhibits proliferation of MV4-11 acute myeloid leukemia (AML) cells expressing FLT3-ITD (IC50 = 25.8 nM). It is selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 μM). Sorafenib N-oxide is also a linear-mixed inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 (Ki = 15 μM in human liver microsomes).

MC4171 (compound 34), a selective KAT8 inhibitor (IC50=8.1 µM), demonstrates moderate antiproliferative activity at micromolar concentrations in various cancer cell lines, such as NSCLC and AML. This property highlights its potential utility in cancer research [1].

UC-764864 is a selective UBE2N inhibitor that blocks E1-UBE2N thioester transfer, inhibits innate immune signaling and induces cytotoxic effects in MDS/AML cell lines and primary cells. In addition, UC-764864 reduces the ubiquitination status of UBE2N and can be used to study leukemia.

KRN383 also inhibited the proliferation of the ITD-positive cell lines with IC(50) values of < or =2.9 nM. A single oral administration of 80 mg/kg of KRN383 eradicated ITD-positive xenograft tumors in nude mice and prolonged the survival of SCID mice carrying ITD-positive AML cells. The effectiveness of a single oral dose of KRN383 suggests that it has the potential to be used in a wide variety of clinical regimens, including multicycle and combination therapies.

LSD1-IN-13 hydrochloride (compound 7e) is an orally active inhibitor of LSD1 (IC50: 24.43 nM). hydrochloride induces differentiation of AML (acute myeloid leukemia) cell lines.

QA-68 (QA-68-ZU81), a potent bromodomain-containing protein 9 (BRD9) degrader, effectively inhibits cell cycle progression and cell colony formation. Demonstrating antiproliferative activity, this compound is particularly effective against acute myeloid leukemia (AML) cell lines [1].

Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib, which is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.

AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.

BCL6-IN-10 (Compound WK499) is an inhibitor of BCL6, disrupting its interaction with the SMRT protein and promoting apoptosis, cell cycle arrest, and DNA damage. It effectively hampers the proliferation of various AML cell lines, with IC50 values of 0.91, 1.63, 1.026, 7.42, 0.87, and 0.85μM for OCI-AML3, THP1, MOLM13, HL60, KG1, and NB4 cells, respectively [1].

FD1024 is a potent PIM inhibitor, displaying inhibitory concentrations (IC50s) of 1.96 nM, 38.9 nM, and 4.17 nM for PIM1, PIM2, and PIM3, respectively. It demonstrates significant antiproliferative effects on several AML cell lines, with IC50 values of 0.16 μM for EOL-1, 0.12 μM for MV-4-11, 1.05 μM for KG-1, and 1.39 μM for MOLM-16. Additionally, FD1024 has shown antitumor efficacy in murine models [1].

FD223 is a potent, selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor with a marked affinity (IC50=1 nM), demonstrating notable selectivity against other isoforms (IC50s: α=51 nM, β=29 nM, γ=37 nM). This compound effectively suppresses the proliferation of acute myeloid leukemia (AML) cell lines by inhibiting p-AKT Ser473, thereby inducing G1 phase cell cycle arrest. FD223 holds promise for leukemia research, particularly in AML[1].

Rohinitib, a potent and specific eIF4A inhibitor, effectively induces apoptosis in acute myeloid leukemia (AML) cell lines and decreases the leukemia burden in AML xenograft models. This compound is utilized in the research of AML.

LGB-321 is a potent and selective ATP-competitive small molecule inhibitor of PIM kinases (Pan-PIM kinase inhibitor). LGB321 is unique relative to previously described PIM inhibitors, in that it is active in PIM2 dependent cell lines. , a kinase that has proven difficult to inhibit in the cellular context. Consistent with its activity on all three PIM kinases, LGB321 inhibits proliferation of a number of cell lines derived from diverse hematological malignancies, including MM, AML, CML and B-Cell NHL. In vivo, LGB-321 is orally available, demonstrates efficacy in tumor xenografts and is well-tolerated within the therapeutic exposure range in mice. (source: Clin Cancer Res. 2014 Apr 1;20(7):1834-45 )

dBRD9 HCl is a PROTAC composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide . dBRD9 HCl is a potent and selective degrader of BRD9 (IC50 = 56.6 nM in MOLM-13 cells). dBRD9 HCl does not degrade BRD4 or BRD7 at concentrations up to 5 μM. dBRD9 HCl displays antiproliferative effects in human AML cell lines.

Antiproliferative agent-30 (Compound 8g) demonstrates broad-spectrum antiproliferative activity, with IC50 values of 0.054 nM, 0.008 nM, and 0.144 nM against HCT-116, K562, and MV-4-11 cancer cell lines, respectively. It inhibits tubulin assembly as well as FLT3 and Abl1 kinases and exhibits vascular-disrupting capabilities. Additionally, it exerts an anticancer effect against acute myeloid leukemia (AML) with FLT3-ITD-TKD mutations [1].

FLT3-IN-20 (compound 34f) is a potent FLT3 inhibitor, demonstrating IC50 values of 1 nM for FLT3-D835Y and 4 nM for FLT3-ITD. It exhibits anti-proliferative effects on FLT3-ITD-positive AML cell lines, with IC50s of 7 nM in MV4-11 and 9 nM in MOLM-13, as well as 4 nM in a MOLM-13 variant harboring the FLT3-ITD-D835Y mutation. FLT3-IN-20 is utilized in cancer research [1].

LSD1-IN-13 (compound 7e) is an orally active LSD1 inhibitor (IC50: 24.43 nM) that also activates CD86 expression (EC50: 470 nM).LSD1-IN-13 induces differentiation of AML (acute myeloid leukaemia) cell lines.

dBRD9 is a PROTAC. dBRD9 is a double-acting molecule, partially containing Bromodomain-containing protein 9 (BRD9), ligand that recruits the cereblon E3 ubiquitin ligase. Ligand that recruits the cereblon E3 ubiquitin ligase. dBRD9 can inhibit the degradation of BRD9 in MOLM-13 cells, and the IC50 is 104 nM.