Tilvestamab (BGB149) is a humanized anti-AXL antibody that blocks AXL-mediated cell signaling. Tilvestamab significantly inhibits Gas6-induced AXL activation in 786-0-Luc RCC cells and inhibits downstream AKT phosphorylation. Tilvestamab can be used in cancer research, particularly in AXL overexpressing renal cell carcinomas[1].
Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM.
Axl/Mer-IN-1 (Compound 1) is an Axl/Mer receptor tyrosine kinase (Axl/Mer RTK) and CSF1R inhibitor with Kds of <0.1 μM[1].
Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models[1].
UNC-1062 is a potent and selective Mer kinase inhibitor with IC50 of 1.1 nM, Ki of 0.33 nM; shows improved selectivity and activity against Mer relative to other TAM family RTKs (78-fold selectivity over Axl and 36-fold over Tyro3); inhibits Mer auto-phosphorylation in human pre-B leukemia 697 cells with IC50 of 6.4 nM, also inhibits colony formation in soft agar in tumor cells.
Cabozantinib is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
Cabozantinib-d6 (XL184-d6) is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively[1][2][3].
Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
Enapotamab is an anti-AXL/UFO reference antibody. Enapotamab can be used to synthesis Bcl-xl inhibitor antibody-drug conjugates[1].
Batiraxcept (AVB-S6-500) is a highly potent and specific AXL inhibitor, a recombinant fusion protein dimer containing the extracellular domain of human AXLM and human immunoglobulin G1 heavy chain (Fc). Batiraxcept binds to GAS6 and inhibits the interaction of GAS6 with AXL, thereby substantially reducing AXL signaled invasion and migration of highly metastatic cells in vitro and inhibiting metastatic disease in nonclinical models of aggressive human cancers. Batiraxcept is available for studies in advanced or metastatic clear cell renal cell carcinoma (ccRCC) and platinum sensitive recurrent ovarian cancer[1][2].
RU-301 is a pan-TAM receptor inhibitor, exerts pan-TAM inhibitory activity by binding at the interface between Gas6 and the Ig1 domain of the respective TAMs with Kd and IC50 values of 12 μM and 10 μM, respectively[1].
PF-07265807 (PF 07265807) is a potent, selective dual Axl/Mer inhibitor, blocks Axl- and Mer-mediated signal transduction pathways, and inhibits proliferation and migration of Axl- and Mer-overexpressing tumor cells.
2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 also inhibits Axl with an IC50 of 0.49 nM.
TP-0903 is a potent and selective Axl receptor tyrosine kinase inhibitor with an IC50 value of 27 nM.
BMS 777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases.
Axl-IN-12 (Example 2) is a potent AXL inhibitor. Axl-IN-12 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals[1].
NPS-1034 is a dual inhibitor of AXL and MET with IC50s of 10.3 and 48 nM, respectively.
Cabozantinib-d4 is deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
TL4830031 (compound 8i), a quinolone antibiotic derivatives, is a potent Axl inhibitor with an IC50 value of 26 nM. TL4830031 inhibits the phosphorylation of Axl. TL4830031 inhibits cell invasion and migration. TL4830031 can be used for cancer research[1].
R916562 is a potential and selective Axl/VEGF-R2 dual inhibitor with IC50s of 136 and 24 nM, respectively.
Axl-IN-11 (Example 1) is a potent AXL inhibitor. Axl-IN-11 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals[1].
AXL-IN-13 is a potent and orally active AXL inhibitor (IC50: 1.6 nM, Kd: 0.26 nM). AXL-IN-13 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion[1].
Mipasetamab uzoptirine (ADCT-601) is an AXL-targeted antibody-drug conjugates (ADCs). Mipasetamab uzoptirine consists of a humanized anti-AXL antibody, a cleavable linker and the potent pyrrolobenzodiazepine (PBD) dimer cytotoxin SG3199. Mipasetamab uzoptirine can be used for the research of cancers[1].
LDC1267 is a highly selective TAM(Tyro3, Axl and Mer) kinase inhibitor with IC50 of <5 nM/8 nM/29 nM for Tyro3,Axl and Mer respectively.IC50 value: <5 nM/8 nM/29 nM(Tyro3/Axl/Mer) [1]Target: TAM kinase inhibitorin vitro: LDC1267 preferentially inhibits Tyro3,Axl andMer at lownanomolarity, as determined by tracer-based binding assays. Treatment of NKG2D activated NK cells with LDC1267 indeed abolished the inhibitory effects of Gas6 stimulation;LDC1267 had no apparent additional effect in Cbl-b-deficient NK cells. in vivo: wild-type mice treated with LDC1267 showed enhanced cytotoxicity towardsRMAcells overexpressing the NKG2D ligand Rae-1 (RMA-Rae1) to the same extent as C373AKI/KI mice, but had no effect on the already enhanced NK cytotoxicity in Cbl-b-mutant mice. Challenged mice with B16F10 melanoma followedby intraperitoneal LDC1267 treatment. LDC1267 markedly reduced metastatic spreading ofmelanomas; NK1.1 depletion abolished the therapeutic benefits of LDC1267.
SGI-7079 is an Axl inhibitor, significantly inhibits the proliferation of SUM149 or KPL-4 cells with an IC50 of 0.43 or 0.16 μM, respectively.Ic50 value:Target: Axlin vitro: SGI-7079 treatment inhibits the phosphorylation of Axl at Tyr 702 upon Gas6 stimulation in SUM149 cells. The growth of SUM149 and KPL-4 in soft agar, one of the hallmark characteristics of cellular transformation and uncontrolled cell growth, is also significantly inhibited by SGI-7079 treatment. SGI-7079 treatment also significantly decreases the migration and invasion of SUM149 cells and the invasion of KPL-4 cells. Taken together, Axl inhibitor SGI-7079 significantly inhibits the proliferation, migration, and invasion of IBC cells, suggesting that Axl may be a promising therapeutic target in patients with IBC. [1]in vivo: SGI-7079 inhibits tumor growth in a dose dependent manner, and at the maximum dose, inhibited tumor growth by 67%, compared to control. The combined inhibition of Axl (SGI-7079) plus EGFR (Erlotinib) is significantly more effective than either drug alone. Notably, SGI-7079 + Erlotinib (25/100 mg/kg) reduced the tumor growth by 82%. Axl blockade by SGI-7079 inhibits the growth of mesenchymal NSCLC xenograft tumors. [2]
Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC)[1][2].
Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis[1].
Gilteritinib hemifumarate is a potent FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.
TAM-IN-2 is a TAM inhibitor extracted from patent US 20170275290 A1, pyrrolotriazine compound 0904[1].
Multi-kinase-IN-1 (Compound 11k) is a potent kinase inhibitor with antitumor activity. Multi-kinase-IN-1 induces cell apoptosis, and can be studied for colorectal cancer[1].