ba/f3

Eltrombopag (SB-497115-GR), an orally active thrombopoietin receptor agonist with megakaryopoiesis stimulating activity, binds to and stimulates the platelet thrombopoietin receptor (TPO-R or CD110).

Eltrombopag Olamine (Eltrombopag diethanolamine salt) is an orally active small-molecule, nonpeptide thrombopoietin receptor agonist that stimulates megakaryopoiesis. It binds to and activates the transmembrane domain of the platelet thrombopoietin receptor (TPO-R or CD110), promoting the proliferation and differentiation of megakaryocytic cells and enhancing platelet production.

NVP-BVU972 is a selective and potent Met inhibitor with IC50 of 14 nM.

Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, with KDs of 0.2, 0.76, 13, and 1.2 nM for EGFR, HER2, BLK, and RIPK2, respectively, and exhibits anticancer activity.

Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

ALK ROS1 inhibitor 2e HCL possesses anti-apoptotic, anti-proliferative and anti-tumour activities.

Butyzamide is an effective and oral Mpl activator. It is a novel non-peptide-based molecule with antagonistic effects on thrombopoietin (TPO) receptors, which promotes proliferation of human Mpl (hMpl) expression and mouse pro B cell line Ba F3. The phosphorylation of JAK2, STAT3, STAT5 and MAPK is induced. Butyzamide has been shown to help increase platelet levels in mouse xenotransplantation trials.

Osimertinib mesylate (AZD-9291 mesylate) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib mesylate has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.

BI-4142 is an orally active, potent and selective HER2 inhibitor that inhibits cancer cell proliferation, suppresses her2-dependent cell lines and inhibits downstream signalling.

AKE-72 is a Pan-BCR-ABL inhibitor with anti-leukemic activity.AKE-72 inhibits the proliferation of Ba/F3 cells expressing natural BCR-ABL or its T315I mutant.

Reslizumab (Sch 55700) is a humanized immunoglobulin G (IgG)4 κ monoclonal antibody that binds to human interleukin 5, thereby decreasing eosinophil production and survival.Reslizumab improves lung function, induces a decrease in eosinophil production and maturation, and may be used in the study of asthma.

HG6-64-1 is a potent and selective inhibitor of B-Raf, with an IC50 of 0.09 μM on B-raf V600E-transformed Ba F3 cells.

JAK3-IN-1 is an orally active, selective and potent JAK3 inhibitor that can be used to study immune system diseases.

(S,R,S)-AHPC TFA (VHL ligand 1 TFA) (VH032-NH2 TFA) is a VH032-based ligand designed for von Hippel-Lindau (VHL) protein recruitment. This compound can be linked to protein ligands (e.g., BCR-ABL1) using a linker to create PROTACs (e.g., GMB-475), which effectively induce the degradation of BCR-ABL1, demonstrated by an IC50 of 1.11 μM in Ba/F3 cells.

MerTK Axl-IN-1 (Compound A-910) is a potent and selective dual inhibitor of MerTK Axl, exhibiting IC50 values of 4.2 nM and 8.8 nM in Ba F3 cells, and 0.2 nM and 0.9 nM in HTRF cells, respectively. It effectively inhibits pMerTK in vivo and possesses a long half-life and high oral bioavailability.

DS06652923 is an orally active inhibitor targeting EGFR triple mutations. It exhibits growth-inhibitory effects on Ba F3EGFRdel19 T90M C795S cells, with a GI50 value of 9.4 nM. Additionally, DS06652923 induces tumor regression in the Ba F3 syngeneic transplantation model.

AZ 14145845, a potent and highly selective dual Mer Axl kinase inhibitor (pIC50 = 7 nM and 7.8 nM in pAxl and pMer, respectively), demonstrates significant efficacy in reducing tumor growth in a dose-dependent manner within the Mer and Axl kinase Ba F3 tumor xenograft model in vivo. When combined with anti-PD1 antibodies and ionizing radiation, this compound enhances survival rates in mice bearing MC38-derived tumors. Additionally, AZ 14145845 is orally bioavailable.

JBJ-07-149 is an inhibitor of EGFRL858R T790M with an IC50 of 1.1 nM. It suppresses the proliferation of Ba F3 cells with IC50 values of 4.9 μM when used alone, and 0.148 μM when combined with Cetuximab. Additionally, JBJ-07-149 can serve as a target protein ligand for synthesizing [DDC-01-163].

EGFR-IN-140 (Compound 31) is an inhibitor of EGFR, effectively targeting both wild-type EGFR and the EGFRL858R T790M C797S mutant, with Ki values of 0.95 nM and 2.1 nM, respectively. Additionally, it inhibits EGFRdel19 T790M C797S in Ba F3 cells with an IC50 of 56.9 nM and demonstrates antitumor activity in mouse models.

JAK-IN-40 (Compound 46) is an inhibitor of JAK, effectively targeting JAK1, JAK2, and JAK3 with IC50 values of 0.022, 0.759, and 1.601 μM, respectively. It reduces the phosphorylation of STAT3 and inhibits the proliferation of cancer cells Ba F3 and JAK1-TEL Ba F3 with GI50 values of 0.614 μM and 0.193 μM. JAK-IN-40 arrests cell cycle progression at the G2 M phase in H1975 and H2087 cells, leading to apoptosis. Additionally, JAK-IN-40 exhibits a synergistic anti-tumor effect when used in combination with Osimertinib.

DA-0157 is an orally active inhibitor targeting EGFR and ALK, designed to overcome resistance mutations in non-small cell lung cancer (NSCLC). It effectively inhibits the proliferation of Ba F3-EGFR Del19 T790M C797S (IC50= 6.9 nM), Ba F3-EGFR WT (IC50= 0.83 μM), Ba F3-EML4-ALK-L1196M (IC50= 5.5 nM), and Ba F3-EML4-ALK (IC50= 7.4 nM). Additionally, DA-0157 inhibits CYP2D6 with an IC50 of 5.26 μM and demonstrates antitumor activity in mouse models.

QZ2135 (compound 20) is a PROTAC degrader that specifically targets RET and exhibits antitumor activity in vivo within a Ba F3-KIF5B-RET-G810C xenograft mouse model. The compound demonstrates degradation activity with DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C) when targeting KIF5B-RET. QZ2135 is composed of the target protein ligand (red part) RETligand-3, the E3 ligase ligand (blue part) Lenalidomide-F, and the PROTAC Linker (black part) 7-Iodohept-1-yne, wherein the target protein ligand combined with the linker forms the conjugate RETLigand-Linker Conjugate-1.

Type II TRK inhibitor 2 (compound 40l) is a selective Type II TRK inhibitor characterized by plasma stability and moderate liver microsome stability. It significantly impedes the proliferation of Km-12, Ba/F3-TRKAG595R, and Ba/F3-TRKAG667C cells with IC50 values of 4.1 nM, 41.5 nM, and 1.4 nM, respectively. Type II TRK inhibitor 2 is applicable for research into NTRK fusion cancers.