UNC2025 HCl

Catalog No.S7576 Synonyms: UNC2025 hydrochloride

For research use only.

UNC2025 HCl 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.

UNC2025 HCl Chemical Structure

CAS No. 2070015-17-5

Selleck's UNC2025 HCl has been cited by 8 Publications

Purity & Quality Control

Choose Selective Axl Inhibitors

Biological Activity

Description UNC2025 HCl 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 NWq1b4xsTnWwY4Tpc44h[XO|YYm= NHftN3gyKGh? NV;IT4ZRUW6qaXLpeIlwdiCxZjDFS2ZTKGW6dILhZ4VtdHWuYYKveJJidnOvZX3idoFv\SCmb33hbY4ufGGpZ3XkJG1meiCrboTyZYNmdGy3bHHyJIRwdWGrbjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckA{OkRiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDFS2Yue3SrbYXsZZRm\CCxZjDwbI9{eGixconsZZRqd25icILleJJm[XSnZDDmc5IhOSCqcjDwdolweiC2bzDFS2Yhe3SrbYXsZZRqd25iYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVIvPyCwTR?= NXXIO2I6OjVyNki4NFA>
697 cells  M4\0XWZ2dmO2aX;uJIF{e2G7 NUDt[mM5OSCq NGmzO4VKdmirYnn0bY9vKG:oIF3ldkBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gOlk4KGOnbHzzJJBz\WmwY4XiZZRm\CCob4KgNUBpeiCkeTDk[Y5{cXSxbXX0dpktKEmFNUC9Nk44KG6P NYPMT5psOjVyNki4NFA>
Molm-14 cells NIfEZ45HfW6ldHnvckBie3OjeR?= NUf1SJUyOSCq MW\Jcohq[mm2aX;uJI9nKE[udEOgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF3vcI0uOTRiY3XscJMheHKnaX7jeYJifGWmIH\vdkAyKGi{IHL5JIRmdnOrdH;t[ZRzgSxiSVO1NF0xNjBzNDFOwG0> MlvWNlUxPjh6MEC=
A549 cells MWHGeY5kfGmxbjDhd5NigQ>? NETYe2Y2OC1|MECgcm0> NXLVOFJMUW6qaXLpeIlwdiCxZjDN[ZIudWWmaXH0[YQh[2:ub375JIZwem2jdHnvckBqdiCqdX3hckBCPTR7IHPlcIx{KGG2IEWwJJRwKDNyMDDuUUBu\WG|dYLl[EBi\nSncjCyJJdm\Wu|IHL5JJNw\nRiYXfhdkBkd2yxbomg[o9zdWG2aX;uJIF{e2G7 NU\PXZE{OjVyNki4NFA>
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 (from reference)

Animal Research:[1]
  • Animal Models: NOD/SCID/gamma mice transplanted with 697 acute leukemia cells
  • Dosages: 3 mg/kg
  • Administration: p.o.

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)

Chemical Information

Molecular Weight 513.12
Formula

C28H41ClN6O

CAS No. 2070015-17-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCCNC1=NC=C2C(=CN(C2=N1)C3CCC(CC3)O)C4=CC=C(C=C4)CN5CCN(CC5)C.Cl

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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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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