产品
编 号：F762406
分子式：C28H41ClN6O
分子量：513.12
分子式：C28H41ClN6O
分子量：513.12
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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2mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 2070015-17-5
产品详情
生物活性：
UNC2025 hydrochloride is a potent, ATP-competitive, and highly orally active 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.
体内研究：
UNC2025 (intravenous injection or oral adminstration; 3 mg/kg) exhibits an excellent PK properties: low clearance (9.2 mL/min kg), longer half-life (3.8 h), and high oral exposure (100%), it shows Tmax, Cmax, and AUClast 0.50 hour, 1.6 μM, and 9.2 h?μM, respectively.UNC2025 (orally adminstration; 50 or 75 mg/kg; 34 and 70 days) mediates a statistically significant dose-dependent reduction in tumor burden relative to vehicle. mediates dose-dependent increases in median survival from 26 days after initiation of treatment in vehicle-treated mice, to 34 and 70 days in mice treated with 50 or 75 mg/kg UNC2025, respectively.Animal Model:NSG mice injected with 697 B-ALL cells
Dosage:50 or 75 mg/kg
Administration:Oral adminstration
Result:Delayed the disease progression.
体外研究：
UNC2025 is against FLT3, MER, AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, KIT and Met with IC50 values of 0.35 nM,0.46 nM, 1.65 nM, 1.67 nM, 4.38nM, 5.75 nM, 5.83 nM, 6.14 nM,7.97 nM , 8.18 nM and 364 nM, respectively.UNC2025 (0-60 nM; 1 hour) mediates potent inhibition of Mer phosphorylation with an IC50?of 2.7 nM?in 697 B-ALL cells.UNC2025 (0-60 nM; 1 hour) results in decreased phosphorylation of Flt3 with an IC50?of 14 nM in Flt3-ITD positive Molm-14 acute myeloid leukemia cells.UNC2025 (3 nM-3 μM; 1 hour) decreases p-MEK, p-AXL, p-TYRO3 expression as a concentration manner in 32D Cells.UNC2025 (14 nM–10 μM; 48 hours) inhibits MERTK signaling and colony-forming potential in a MERTK-expressing patient sample with a 20-fold difference in sensitivity of MERTK-expressing leukemia blasts relative to normal cord or marrow blood mononuclear cells.UNC2025 (25-300 nM; 1 hour) mediates potent and dose-dependent decreases in MERTK phosphorylation/activation in both cell lines and inhibition of MERTK correlated with decreased phosphorylation of previously reported MERTK-dependent signaling components STAT6, AKT, and ERK1/2.
UNC2025 hydrochloride is a potent, ATP-competitive, and highly orally active 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.
体内研究：
UNC2025 (intravenous injection or oral adminstration; 3 mg/kg) exhibits an excellent PK properties: low clearance (9.2 mL/min kg), longer half-life (3.8 h), and high oral exposure (100%), it shows Tmax, Cmax, and AUClast 0.50 hour, 1.6 μM, and 9.2 h?μM, respectively.UNC2025 (orally adminstration; 50 or 75 mg/kg; 34 and 70 days) mediates a statistically significant dose-dependent reduction in tumor burden relative to vehicle. mediates dose-dependent increases in median survival from 26 days after initiation of treatment in vehicle-treated mice, to 34 and 70 days in mice treated with 50 or 75 mg/kg UNC2025, respectively.Animal Model:NSG mice injected with 697 B-ALL cells
Dosage:50 or 75 mg/kg
Administration:Oral adminstration
Result:Delayed the disease progression.
体外研究：
UNC2025 is against FLT3, MER, AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, KIT and Met with IC50 values of 0.35 nM,0.46 nM, 1.65 nM, 1.67 nM, 4.38nM, 5.75 nM, 5.83 nM, 6.14 nM,7.97 nM , 8.18 nM and 364 nM, respectively.UNC2025 (0-60 nM; 1 hour) mediates potent inhibition of Mer phosphorylation with an IC50?of 2.7 nM?in 697 B-ALL cells.UNC2025 (0-60 nM; 1 hour) results in decreased phosphorylation of Flt3 with an IC50?of 14 nM in Flt3-ITD positive Molm-14 acute myeloid leukemia cells.UNC2025 (3 nM-3 μM; 1 hour) decreases p-MEK, p-AXL, p-TYRO3 expression as a concentration manner in 32D Cells.UNC2025 (14 nM–10 μM; 48 hours) inhibits MERTK signaling and colony-forming potential in a MERTK-expressing patient sample with a 20-fold difference in sensitivity of MERTK-expressing leukemia blasts relative to normal cord or marrow blood mononuclear cells.UNC2025 (25-300 nM; 1 hour) mediates potent and dose-dependent decreases in MERTK phosphorylation/activation in both cell lines and inhibition of MERTK correlated with decreased phosphorylation of previously reported MERTK-dependent signaling components STAT6, AKT, and ERK1/2.
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