UNC2025

Catalog No.S7576

UNC2025 Chemical Structure

Molecular Weight(MW): 513.12

UNC2025 is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.

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Biological Activity

Description UNC2025 is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.
Targets
Mer [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
Axl [1]
(Cell-free assay)
Tyro3 [1]
(Cell-free assay)
0.74 nM 0.8 nM 14 nM 17 nM
In vitro

In 697 B-ALL cells, UNC-2025 potently inhibits Mer phosphorylation with IC50 of 2.7 nM. In A549 NSCLC and Molm-14 AML cell lines, UNC-2025 causes significant inhibition of colony formation dependent on Mer8 and Flt3. [1] In H2228 and H1299 cell lines, UNC-2025 inhibits MERTK oncogenic signaling downstream, such as basal and stimulated pAKT and pERK1/2. In four NSCLC cell lines, UNC-2025 also induces apoptotic cell death, and decreases colony formation. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
32D cells M4DnRmZ2dmO2aX;uJIF{e2G7 NHjqTnEyKGh? NWDGZ|MzUW6qaXLpeIlwdiCxZjDFS2ZTKGW6dILhZ4VtdHWuYYKveJJidnOvZX3idoFv\SCmb33hbY4ufGGpZ3XkJG1meiCrboTyZYNmdGy3bHHyJIRwdWGrbjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckA{OkRiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDFS2Yue3SrbYXsZZRm\CCxZjDwbI9{eGixconsZZRqd25icILleJJm[XSnZDDmc5IhOSCqcjDwdolweiC2bzDFS2Yhe3SrbYXsZZRqd25iYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVIvPyCwTR?= NFjLbVMzPTB4OEiwNC=>
697 cells  MmLPSpVv[3Srb36gZZN{[Xl? MVexJIg> M2LJWGlvcGmkaYTpc44hd2ZiTXXyJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjC2PVch[2WubIOgdJJmcW6ldXLheIVlKG[xcjCxJIhzKGK7IHTlcpNqfG:vZYTyfUwhUUN3ME2yMlchdk1? MXWyOVA3QDhyMB?=
Molm-14 cells MUHGeY5kfGmxbjDhd5NigQ>? NFi4UIgyKGh? NGThU5BKdmirYnn0bY9vKG:oIF\seFMheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1wdG1vMUSgZ4VtdHNicILlbY5kfWKjdHXkJIZweiBzIHjyJIJ6KGSnboPpeI9u\XS{eTygTWM2OD1yLkCxOEDPxE1? MknHNlUxPjh6MEC=
A549 cells MYHGeY5kfGmxbjDhd5NigQ>? NHvGS2s2OC1|MECgcm0> NUXDSnU3UW6qaXLpeIlwdiCxZjDN[ZIudWWmaXH0[YQh[2:ub375JIZwem2jdHnvckBqdiCqdX3hckBCPTR7IHPlcIx{KGG2IEWwJJRwKDNyMDDuUUBu\WG|dYLl[EBi\nSncjCyJJdm\Wu|IHL5JJNw\nRiYXfhdkBkd2yxbomg[o9zdWG2aX;uJIF{e2G7 MX6yOVA3QDhyMB?=

... Click to View More Cell Line Experimental Data

In vivo In mice bearing 697 acute leukemia tumors, UNC-2025 (3 mg/kg, p.o.) shows good solubility and DMPK properties, and results in effective target inhibition. [1] In mice bearing H2228 or A549 tumors, UNC-2025 (50 mg/kg, p.o.) inhibits tumor growth. [2]

Protocol

Animal Research:[1]
- Collapse
  • Animal Models: NOD/SCID/gamma mice transplanted with 697 acute leukemia cells
  • Formulation: Suspended in 0.5% (w/v) NaCMC with 0.1% (v/v) Tween-80 in water
  • Dosages: 3 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro Water 100 mg/mL (194.88 mM)
DMSO 25 mg/mL warmed (48.72 mM)
Ethanol 8 mg/mL warmed (15.59 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 513.12
Formula

C28H41ClN6O

CAS No. 1429881-91-3(free base)
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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TAM Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID