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Chemical Structure| 1429881-91-3 Chemical Structure| 1429881-91-3

Structure of UNC2025
CAS No.: 1429881-91-3

Chemical Structure| 1429881-91-3

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UNC2025 is an inhibitor of Mer and Flt3 with IC50 of 0.8 nM and 0.74 nM, respectively.

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Product Details of UNC2025

CAS No. :1429881-91-3
Formula : C28H40N6O
M.W : 476.66
SMILES Code : O[C@H]1CC[C@H](N2C=C(C3=CC=C(CN4CCN(C)CC4)C=C3)C5=CN=C(NCCCC)N=C52)CC1
MDL No. :MFCD28142874
InChI Key :MJSHVHLADKXCML-UHFFFAOYSA-N
Pubchem ID :73425588

Safety of UNC2025

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of UNC2025

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
G361 1000 nM 90 minutes inhibition of MERTK activation and downstream signaling Mol Cancer Ther. 2019 Feb;18(2):278-288.
J774 134 nM 5 days Evaluate the inhibitory effect of UNC2025 on J774 cell growth, with an IC50 of 134 nM. Neuro Oncol. 2018 Jan 10;20(1):92-102.
EOC 2 199 nM 5 days Evaluate the inhibitory effect of UNC2025 on EOC 2 cell growth, with an IC50 of 199 nM. Neuro Oncol. 2018 Jan 10;20(1):92-102.
GSC20 1.5 µM 5 days Evaluate the inhibitory effect of UNC2025 on GSC20 cell growth, with an IC50 of 1.5 µM. Neuro Oncol. 2018 Jan 10;20(1):92-102.
GSC11 86 nM 5 days Evaluate the inhibitory effect of UNC2025 on GSC11 cell growth, with an IC50 of 86 nM. Neuro Oncol. 2018 Jan 10;20(1):92-102.
MeWo 100 nM 72 hours reduction in survivin levels Mol Cancer Ther. 2019 Feb;18(2):278-288.
A101D 50 nM 10 days reduction in colony formation Mol Cancer Ther. 2019 Feb;18(2):278-288.
HMCB 300 nM 90 minutes inhibition of MERTK activation and downstream signaling Mol Cancer Ther. 2019 Feb;18(2):278-288.
TRP 231.6 nM 5 days Evaluate the inhibitory effect of UNC2025 on TRP cell growth, with an IC50 of 231.6 nM. Neuro Oncol. 2018 Jan 10;20(1):92-102.
AML-123009 patient sample 25-300nM 48 hours Inhibited colony formation, >90% inhibition at 300nM Clin Cancer Res. 2017 Mar 15;23(6):1481-1492.
NOMO-1 AML cells 200-300nM 48 hours Induced cell death, 25-90% of cells died after 48-hour treatment Clin Cancer Res. 2017 Mar 15;23(6):1481-1492.
Jurkat T-ALL cells 200-300nM 48 hours Induced cell death, 25-90% of cells died after 48-hour treatment Clin Cancer Res. 2017 Mar 15;23(6):1481-1492.
Kasumi-1 AML cells 200-300nM 48 hours Induced cell death, 25-90% of cells died after 48-hour treatment Clin Cancer Res. 2017 Mar 15;23(6):1481-1492.
697 B-ALL cells 200-300nM 48 hours Induced cell death, 25-90% of cells died after 48-hour treatment Clin Cancer Res. 2017 Mar 15;23(6):1481-1492.
M2 macrophages 1 µg/mL 2 hours Inhibit MerTK phosphorylation and block efferocytosis of apoptotic cells Nat Commun. 2023 Mar 25;14(1):1675.
Schwannoma cells 0.03-6.0 μM 72 hours and 7 days UNC2025 decreased the total number of schwannoma cells, increased the number of dead cells, and reduced the proliferation of Ki67-positive cells. Oncogene. 2024 Oct;43(41):3049-3061.
Meningioma cells 0.03-6.0 μM 72 hours and 7 days UNC2025 decreased the total number of meningioma cells, increased the number of dead cells, and reduced the proliferation of Ki67-positive cells. Oncogene. 2024 Oct;43(41):3049-3061.
Murine washed platelets 0.5 µM 15 minutes inhibited collagen-stimulated platelet aggregation J Thromb Haemost. 2018 Feb;16(2):352-363.
Human platelet rich plasma (PRP) 5 µM 15 minutes inhibited collagen-stimulated platelet aggregation J Thromb Haemost. 2018 Feb;16(2):352-363.
Human washed platelets (WP) 0.5 µM 15 minutes inhibited collagen-stimulated platelet aggregation J Thromb Haemost. 2018 Feb;16(2):352-363.
Meningioma cells 1 µM 72 hours To evaluate the effect of UNC2025 on meningioma spheroid viability, results showed UNC2025 significantly decreased spheroid viability. Acta Neuropathol Commun. 2023 Dec 15;11(1):198.
H1299 300 nM 72 hours To assess the effect of UNC2025 on apoptosis, results showed UNC2025 significantly increased apoptosis. Mol Cancer Ther. 2015 Sep;14(9):2014-22.
Colo699 300 nM 72 hours To assess the effect of UNC2025 on apoptosis, results showed UNC2025 significantly increased apoptosis. Mol Cancer Ther. 2015 Sep;14(9):2014-22.
A549 300 nM 72 hours To assess the effect of UNC2025 on apoptosis, results showed UNC2025 significantly increased apoptosis. Mol Cancer Ther. 2015 Sep;14(9):2014-22.
H2228 300 nM 72 hours To assess the effect of UNC2025 on apoptosis, results showed UNC2025 significantly increased apoptosis. Mol Cancer Ther. 2015 Sep;14(9):2014-22.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID/gamma mice Human leukemia xenograft model Oral 3 mg/kg Single dose, bone marrow cells collected 30 minutes later To evaluate the inhibitory effect of UNC2025 on Mer phosphorylation in vivo, results showed significant reduction in Mer phospho-protein levels J Med Chem. 2014 Aug 28;57(16):7031-41.
Nude mice Subcutaneous xenograft model Oral gavage 30 mg/kg or 50 mg/kg Twice daily for several weeks To assess the effect of UNC2025 on tumor growth, results showed UNC2025 significantly inhibited tumor growth. Mol Cancer Ther. 2015 Sep;14(9):2014-22.
Mice TRP allograft model Oral gavage 65 mg/kg Once daily starting from day 7 Evaluate the effect of UNC2025 alone or in combination with radiotherapy on the survival of TRP allograft model mice. Results showed that UNC2025 alone did not significantly prolong survival, but when combined with radiotherapy, 19.4% of mice survived more than 60 days, with complete tumor regression in some mice. Neuro Oncol. 2018 Jan 10;20(1):92-102.
Nude mice MHH-ES-1 xenograft model Intraperitoneal injection 10 mg/kg Every 3 days for 28 days UNC2025 enhanced irinotecan's suppression of tumor growth Nat Commun. 2024 Jun 21;15(1):5292.
NSG mice 697 B-ALL xenograft model Oral 50-75mg/kg Once daily, continuous treatment Significantly reduced tumor burden, median survival increased from 26 days to 70 days Clin Cancer Res. 2017 Mar 15;23(6):1481-1492.
C57BL/6 mice B16F10 melanoma model Peritumoral injection 2.7 µg/mouse Every 3 days for two times Inhibit tumor growth and metastasis, enhance antitumor immune responses Nat Commun. 2023 Mar 25;14(1):1675.
Mice FeCl3-Induced Carotid Artery Thrombosis model Intravenous injection 3 mg/kg Single dose, circulated for 30 minutes Prolonged time to initial clot formation and decreased thrombus stability J Thromb Haemost. 2018 Feb;16(2):352-363.
Male C57BL/6 mice Hepatic ischemia-reperfusion injury model Intravenous injection 50 mg/kg Single dose, followed by reperfusion for up to 6 or 24 hours UNC2025 significantly inhibited MSC-EVs-induced phagocytosis of apoptotic cells by macrophages and increased liver injury Cell Death Discov. 2024 Sep 10;10(1):401
Nude mice BRAF-mutated patient-derived xenograft model Oral gavage 50 mg/kg Twice daily for 50 days Significantly reduced tumor growth Mol Cancer Ther. 2019 Feb;18(2):278-288.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.49mL

2.10mL

1.05mL

20.98mL

4.20mL

2.10mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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