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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
48 Results for "
MerTK
" in MedChemExpress (MCE) Product Catalog:
Products (48)
48 Results for "MerTK" in MCE Product Catalog:
10
10 Publications Verification
Target:
Forschungsgebiete:
LDC1267 is a AXL/TAM/FLT3 inhibitor with IC50 values of 42 nM, 130 nM, and 63 nM against AXL, MERTK, and TYRO3, respectively. LDC1267 blocks GAS6-induced AXL phosphorylation and the downstream AKT/ERK1/2 signaling pathway. LDC1267 inhibits cancer cell proliferation, colony formation, and glioblastoma cell invasion, without causing obvious impairment of cytotoxic autophagic flux. LDC1267 exerts a synergistic effect when used in combination with Imatinib (HY-15463) in chronic myeloid leukemia models. LDC1267 can be widely applied in studies related to glioblastoma and chronic myeloid leukemia .
9
9 Cited Publications
Target:
Forschungsgebiete:
UNC2025 is a potent, ATP-competitive, highly orally active and BBB-permeable Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia .
9
9 Cited Publications
UNC2025 hydrochloride is a potent, ATP-competitive, highly orally active and BBB-permeable Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia .
6
6 Cited Publications
Synonyms: LY2801653
Forschungsgebiete:
Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib (LY2801653) also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM) .
6
MRX-2843 (UNC2371) is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively .
6
6 Cited Publications
Synonyms: LY2801653 dihydrochloride
Forschungsgebiete:
Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM) .
2
2 Cited Publications
Forschungsgebiete:
UNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC50 of 1.1 nM (Morrison Ki = 0.33 nM). UNC1062 exhibits good selectivity for the TAM family (TYRO3 IC50 = 60 nM, AXL IC50 = 85 nM). UNC1062 exhibits significant anti-proliferative effects and induces apoptosis in various cancer models (such as melanoma, gastric cancer, and acute myeloid leukemia). UNC1062 inhibits multiple pathways, including MAPK/ERK, PI3K/AKT and JAK/STAT and affects the motility of head and neck squamous cell carcinoma (HNSCC) cells through the RhoA signaling pathway. UNC1062 inhibits macrophage efferocytosis, and it suitable for research on atherosclerosis .
1
1 Cited Publications
Target:
Forschungsgebiete:
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 .
Forschungsgebiete:
UNC5293 is a MERTK-selective and potent inhibitor (Ki=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 .
Art. -Nr.: HY-173268
CAS. Nr.: 3051784-94-9
Target:
Forschungsgebiete:
UNC9426 is a potent and selective TYRO3 inhibitor (IC50 = 2.1 nM), demonstrating 276-fold and 90-fold selectivity over MERTK and AXL, respectively. UNC9426 reduces platelet aggregation without increasing bleeding time and blocks TYRO3-dependent functions in tumor cells and macrophages. UNC9426 demonstrates a favorable safety profile with no significant increase in bleeding risk in vivo. UNC9426 can be used for functional studies of TYRO3-dependent phenotypes such as non-small cell lung cancer (NSCLC) .
Synonyms: ARRY-067
Target:
Forschungsgebiete:
PF-07265807 (ARRY-067) is a kinase inhibitor with primary targets AXL, MERTK, and TYRO3. PF-07265807 acts as an immunomodulator that cross-activates CD8 + T cells by enhancing dendritic cell function. PF-07265807 blocks downstream signal transduction of AXL and MERTK, and inhibits the proliferation and migration of tumor cells with high expression of these two kinases. PF-07265807 is applicable to research related to advanced or metastatic solid tumors, such as colorectal cancer .
Art. -Nr.: HY-115778
CAS. Nr.: 2011034-35-6
Target:
Forschungsgebiete:
UNC3133 is an orally active, limitedly selective MerTK inhibitor with an IC50 of 3.0 nM. UNC3133 inhibits Axl, Tyro3 and Flt3 kinases, with IC50 values of 17 nM, 31 nM and 6.8 nM, respectively. UNC3133 is applicable to the research of inflammatory diseases and cancers .
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Forschungsgebiete:
UNC4203 is a potent, orally available and highly selective MERTK inhibitor, with IC50s of 1.2 nM, 140 nM, 42 nM and 90 nM for MERTK, AXL, TYRO3 and FLT3, respectively .
Art. -Nr.: HY-N9454
CAS. Nr.: 91893-83-3
Art. -Nr.: HY-173400
Target:
Forschungsgebiete:
UNC8212 is a TAM kinase inhibitor. UNC8212 has potent inhibitory activity against MERTK and AXL (IC50: 1.5 nM and 1.3 nM, respectively), and also inhibits TYRO3 (IC50: 6.7 nM). UNC8212 mediates polypharmacological properties by targeting the structurally diverse "back pocket" region of the TAM kinase family. UNC8212 binds tightly to TAM kinases and potently inhibits MERTK and AXL phosphorylation. UNC8212 has anti-tumor effects and can be used in cancer immunotherapy and tumor cell targeting research .
Art. -Nr.: HY-174160
Target:
Forschungsgebiete:
MerTK-IN-2 (compound 15f) is an orally active MerTK inhibitor with an IC50 of 37.5 nM. MerTK-IN-2 can induce apoptosis. MerTK-IN-2 has antitumor activity with IC50 values of 1.79, 18.32, and 2.18 μM for human ovarian cancer cells A2780, breast cancer cells MDA-MB-231, and colon cancer cells HCT116, respectively .
Art. -Nr.: HY-172796
CAS. Nr.: 3091640-25-1
Target:
Forschungsgebiete:
UNC9435 (compound 44) is a dual inhibitor of TYRO3/MERTK with IC50 values of 3.7 nM and 1.1 nM, respectively. UNC9435 reduces colony formation in non-small cell lung cancer cultures
Art. -Nr.: HY-176482
CAS. Nr.: 3029898-85-6
Target:
Forschungsgebiete:
MerTK-IN-3 (compound 11) is an orally active and selectivity MerTK inhibitor with IC50 values of 21.5 nM and 991.3 nM for MerTK and Tyro3, respectively. MerTK-IN-3 can be used for study of colon cancer .
Art. -Nr.: HY-169208
CAS. Nr.: 3036376-10-7
Target:
Forschungsgebiete:
MerTK-IN-1 (compund 31) is a MerTK inhibitor with in vivo target binding ability .
Art. -Nr.: HY-162940
CAS. Nr.: 3036009-40-9
Target:
Forschungsgebiete:
MerTK/Axl-IN-1 (Compound A-910) is a potent and selective dual MerTK/Axl inhibitor, with IC50s of 4.2 and 8.8 nM in Ba/F3, and 0.2 and 0.9 nM in HTRF. MerTK/Axl-IN-1 results in pMerTK inhibition in vivo. MerTK/Axl-IN-1 has long half-life, high oral exposure and bioavailability .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
