ba/f3 cells

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.

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.

BI-2865 is a non-covalent pan-KRAS inhibitor.BI-2865 binds to KRAS WT, G12C, G12D, G12V, and G13D mutants with KD values of 6.9, 4.5, 32, 26, and 4.3 nM, respectively.BI-2865 showed antiproliferative activity in BaF3 cells expressing KRAS G12C, G12D, or G12V mutants[1] . BI-2865 showed antiproliferative activity on BaF3 cells expressing KRAS G12C, G12D or G12V mutants, with an average IC50 value of approximately 140 nM.[1]

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).

Imatinib (STI571) is a multi-targeted receptor tyrosine kinase inhibitor that selectively inhibits the kinase activities of BCR/ABL, v-Abl, PDGFR, and c-kit with oral activity. Imatinib has antitumor activity for the treatment of chronic granulocytic leukemia.

SCH-336 is a CB2 receptor agonist (Ki-1.8 nM, EC50-2 nM) with effective, selective, and oral activity. SCH-336 is also bioactive against CB1 receptor, and is 100 times more selective to CB2 receptor than CB1. SCH-336 reduced the binding of guanosine 5' -3-o -(sulfur) triphosphate to the membrane containing hCB, inhibited BaF3/CB2 cell migration, inhibited leukocyte migration in mouse delayed hypersensitivity models, and inhibited antigen-induced pulmonary eosinophilia in mouse allergy models.

Homoharringtonine (HHT) is a natural alkaloid that inhibits the translation of proteins and is cytotoxic. Homoharringtonine acts on the ribosomes of tumor cells to inhibit the elongation step of protein translation, thereby inhibiting protein synthesis, and has antitumor activity.

SHP099 (SHP099 free base) free base is an effective, selective, orally bioavailable, and efficacious SHP2 inhibitor (IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM). SHP099 shows dose-dependent pathway inhibition and antitumor activity in xenograft models.

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

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.

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.

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.

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.

D-65476 is a type III receptor tyrosine kinase (Flt3) inhibitor. It inhibits the proliferation of TEL-Flt3 transfected BA/F3 cells in the absence of IL-3, with an IC50 of 0.2 μM, and is useful for researching Flt3-driven leukemia.

ZSH-2117 is a covalent and selective EGFR PROTAC degrader, with a DC50 of 45 nM in Ba/F3-EGFR[L858R/T790M/C797S] cells. It significantly inhibits cell proliferation and reduces AKT and ERK protein levels in downstream EGFR signaling pathways. ZSH-2117 effectively suppresses tumor growth in Ba/F3-EGFR[L858R/T790M/C797S] xenograft mouse models.

TRK-IN-31 hydrochloride is an orally active TRK inhibitor with an IC50 of 1.8 nM. It demonstrates excellent antiproliferative activity in Ba/F3-MPRIP-TRKAG667C cells and selectively inhibits TRK kinase activity. Additionally, TRK-IN-31 hydrochloride significantly suppresses tumor growth in a Ba/F3-MPRIP-TRKAG667C subcutaneous mouse model.

TRK-IN-31 is an orally active TRK inhibitor with an IC50 of 1.8 nM. It demonstrates excellent antiproliferative activity in Ba/F3-MPRIP-TRKAG667C cells and selectively inhibits TRK kinase activity effectively. TRK-IN-31 also significantly suppresses tumor growth in a Ba/F3-MPRIP-TRKAG667C subcutaneous tumor mouse model.