TAM Receptor Inhibitor

TAM Receptor Inhibitors (101):

Cat. No.	Product Name	Effect	Purity

HY-15150

Bemcentinib	Inhibitor	99.92%
Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC₅₀ of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer.

HY-13016

Cabozantinib	Inhibitor	99.97%
Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC₅₀ values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC₅₀=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.

HY-12432

Gilteritinib	Inhibitor	99.84%
Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC₅₀s of 0.29 nM/0.73 nM, respectively.

HY-114166

2-D08	Inhibitor	99.37%
2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 also inhibits Axl with an IC₅₀ of 0.49 nM.

HY-12076

BMS 777607	Inhibitor	99.36%
BMS 777607 (BMS 817378) 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.

HY-122601

TAM-IN-1	Inhibitor
TAM-IN-1 (compound 1) is a potent macrocyclic inhibitor of Axl and Mer, with K_is of 130 pM and <50 pM, respectively.

HY-P992231

Anti-GAS6 Antibody (KM5321)	Inhibitor
Anti-GAS6 Antibody (KM5321) is a humanized anti-GAS6 monoclonal antibody. Its isotype control is Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).

HY-179535

Axl-IN-21	Inhibitor
Axl-IN-21 is an orally active and selective AXL inhibitor (K_d = 2.7 nM, IC₅₀ = 4.0 nM). Axl-IN-21 displays kinase selectivity and retains strong activity against cancer-related mul-kinases (Mer with K_d = 1.4 nM, DDR1 with IC₅₀ = 22.2 nM, HIPK4 with K_d = 11.0 nM and LOK with K_d =10 nM). Axl-IN-21 overcomes tumor microenvironment-driven resistance by blocking CAF-derived GAS6-induced AXL/STAT3/ABCG1 signaling, restoring chemosensitivity and inhibiting drug efflux in gastric cancer (GC). Axl-IN-21 suppresses TGF-β1-induced epithelial-mesenchymal transition (EMT), migration, and invasion in MDA-MB-231 cells. Axl-IN-21 exhibits no significant cytotoxicity in non-cancerous cells. Axl-IN-21 can be research for triple negative breast cancer and gastric cancer^[1]^[2].

HY-15797

UNC2250	Inhibitor	99.92%
UNC2250 is a potent and selective Mer inhibitor with an IC₅₀ of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.

HY-138696

Zanzalintinib	Inhibitor	99.91%
Zanzalintinib (XL092) is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC₅₀s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. Zanzalintinib exhibits anti-tumor activity. Zanzalintinib has the potential for kinase-dependent diseases and conditions research.

HY-12494

LDC1267	Inhibitor	99.64%
^{LDC1267 is a highly selective TAM (Tyro3, Axl and Mer) kinase inhibitor with IC₅₀s of <5 nM/8 nM/29 nM for Tyro3,Axl and Mer respectively.}

HY-12963

Dubermatinib	Inhibitor	99.84%
Dubermatinib (TP-0903) is a potent and selective Axl receptor tyrosine kinase inhibitor with an IC₅₀ value of 27 nM.

HY-117596

UNC569	Inhibitor	99.92%
UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC₅₀ of 2.9 nM and a K_i of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC₅₀s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors research

HY-132200

UNC5293	Inhibitor	99.93%
UNC5293 is a MERTK-selective and potent inhibitor (K_i=190 pM). UNC5293 inhibits MERTK (IC₅₀=0.9 nM) and is more selective over Axl, Tyro3 and Flt3. UNC5293 exhibits excellent mouse PK properties and is used for bone marrow leukemia research.

HY-12432A

Gilteritinib hemifumarate	Inhibitor	99.75%
Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC₅₀ of 0.29 nM/0.73 nM, respectively.

HY-125510

UNC2541	Inhibitor	99.71%
UNC2541 is a potent and Mer tyrosine kinase (MerTK)-specific inhibitor, binds in the MerTK ATP pocket, with an IC₅₀ of 4.4 nM, more selective over Axl, Tyro3 and Flt3. UNC2541 inhibits phosphorylated MerTK (pMerTK; EC₅₀, 510 nM). UNC2541 abolishes the analgesic and anti-inflammatory effects of ozone in vivo and in vitro.

HY-114358

Tamnorzatinib	Inhibitor	98.59%
Tamnorzatinib (ONO-7475) is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. Tamnorzatinib sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. Tamnorzatinib combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).

HY-100946

CEP-40783	Inhibitor	99.61%
CEP-40783 is a potent, selective and orally available inhibitor of AXL and c-Met with IC₅₀ values of 7 nM and 12 nM, respectively.

HY-119039

RU-301	Inhibitor	99.75%
RU-301 is a pan TAM inhibitor that blocks Gas6-induced TAM activation and tumorigenicity. RU-301 significantly reduces nonalcoholic steatohepatitis (NASH) fibrosis, along with attenuates ERK activation and TGFβ1 expression. RU-301 can be used in studies of cancer and nonalcoholic steatohepatitis.

HY-12964

SGI-7079	Inhibitor	99.32%
SGI-7079 is a selective, ATP-competitive, orally active inhibitor of the receptor tyrosine kinase Axl. SGI-7079 blocks Axl-mediated signaling pathways such as NF-κB activation and MMP-9 expression, thereby inhibiting tumor cell proliferation, migration and invasion. SGI-7079 is mainly used in the research of malignant tumors such as inflammatory breast cancer and bladder cancer, as well as in combination with immunization (used in combination with PD-1 therapy)[1][2][3].

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