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UNC-2025
CAS No. 1429881-91-3
UNC-2025( UNC2025, UNC2025, UNC 2025 )
Catalog No. M17294 CAS No. 1429881-91-3
UNC-2025（ IC50 of 0.74 nM and 0.8 nM） is a potent and orally bioavailable dual MER/FLT3 inhibitor. UNC-2025 is about 20-fold selectivity higher than Axl and Tyro3.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 30 | In Stock |
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| 5MG | 47 | In Stock |
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| 10MG | 77 | In Stock |
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| 25MG | 113 | In Stock |
|
| 50MG | 186 | In Stock |
|
| 100MG | 332 | In Stock |
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| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameUNC-2025
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NoteResearch use only, not for human use.
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Brief DescriptionUNC-2025（ IC50 of 0.74 nM and 0.8 nM） is a potent and orally bioavailable dual MER/FLT3 inhibitor. UNC-2025 is about 20-fold selectivity higher than Axl and Tyro3.
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DescriptionUNC-2025 is a novel potent and highly orally bioavailable Mer/FLT3 dual inhibitor, capable of inhibiting Mer phosphorylation in vivo, following oral dosing as demonstrated by pharmaco-dynamic (PD) studies examining phospho-Mer in leukemic blasts from mouse bone marrow. Kinome profiling versus more than 300 kinases in vitro and cellular selectivity assessments demonstrate that UNC-2025 has similar subnanomolar activity against Flt3, an additional important target in acute myelogenous leukemia (AML), with pharmacologically useful selectivity versus other kinases examined.
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In VitroWestern Blot Analysis Cell Line:32D CellsConcentration:0 nM, 3 nM, 10 nM, 20 nM, 30 nM, 100 nM, 1000 nM, 3000 nM Incubation Time:1 hour Result:Inhibited p-MEK, p-AXL, p-TYRO3 expression Cell Viability Assay Cell Line:Mononuclear cells?Concentration:14 nM–10μM Incubation Time:48 hourResult:Showed IC50 values ranged from 9.0 nM to >10μ M with a median IC50 of 2.38 μM.Western Blot Analysis Cell Line:MERTK-expressing B-cell and T-cell acute lymphoid leukemia (B-ALL and T-ALL) and acute myeloid leukemia (AML) cell lines Concentration:25-300 nM Incubation Time:1 hour Result:Decresed p-MERTK, p-STAT6, p- AKT and p-ERK1/2 expression as a dose-dependent manner.
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In Vivo——
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SynonymsUNC2025, UNC2025, UNC 2025
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PathwayMembrane Transporter/Ion Channel
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TargetTRP/TRPV Channel
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RecptorFLT3| AXL| Mer| Tyro3
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number1429881-91-3
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Formula Weight513.12
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Molecular FormulaC28H41ClN6O
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Purity>98% (HPLC)
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SolubilityDMSO : 33.33 mg/mL. 69.92 mM;
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SMILESCCCCNc1ncc2c(cn(c2n1)[C@H]1CC[C@@H](CC1)O)c1ccc(cc1)CN1CCN(CC1)C.Cl.Cl
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Chemical Name(1r,4r)-4-(2-(butylamino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Zhang W, et al. J Med Chem. 2014, 57(16), 7031-7041.
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