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| 25mg |
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Purity: ≥98%
UNC-2025 is a novel, potent and orally bioavailable dual inhibitor of MER/FLT3 with IC50 of 0.74 nM and 0.8 nM, respectively, it displayed about 20-fold selectivity over Axl and Tyro3. Pharmacodynamic studies (PD) looking at phospho-Mer in leukemic blasts from mouse bone marrow show that UNC-2025 can inhibit Mer phosphorylation in vivo after oral dosing. UNC-2025 has similar subnanomolar activity against Flt3, an additional important target in acute myelogenous leukemia (AML), with pharmacologically useful selectivity compared to other kinases examined, according to kinome profiling versus more than 300 kinases in vitro and cellular selectivity assessments.
| Targets |
FLT3 (IC50 = 0.35 nM); Mer (IC50 = 0.46 nM); Axl (IC50 = 1.65 nM); TrkA (IC50 = 1.67 nM); TrkC (IC50 = 4.38 nM)
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| ln Vitro |
UNC2025 has comparable subnanomolar activity against Flt3, an additional crucial target in acute myelogenous leukemia (AML), with pharmacologically useful selectivity versus other kinases investigated, according to kinome profiling versus more than 300 kinases in vitro and cellular selectivity assessments.[1]
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| ln Vivo |
UNC2025 is a potent and highly oral bioavailable Mer inhibitor that, by pharmacodynamic (PD) studies looking at phospho-Mer in leukemic blasts from mouse bone marrow, is able to inhibit Mer phosphorylation in vivo after oral dosing.[1]
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| Enzyme Assay |
UNC2025 hydrochloride has an IC50 of 0.8/0.74 nM for Mer/Flt3, making it a strong and orally bioavailable dual inhibitor of Mer/Flt3. Studies using pharmacodynamic (PD) methods to look at phospho-Mer in leukemic blasts from mouse bone marrow showed that UNC2025 could inhibit Mer phosphorylation in vivo after oral dosing. The results of kinome profiling against over 300 kinases in vitro and cellular selectivity assessments show that 11 has pharmacologically useful selectivity compared to other kinases examined and has similar subnanomolar activity against Flt3, an additional important target in acute myelogenous leukemia (AML).
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| Cell Assay |
UNC-2025 has a 2.7 nM IC50 and can potently inhibit Mer phosphorylation in 697 B-ALL cells. UNC-2025, which is reliant on Flt3 and Mer8, significantly inhibits colony formation in A549 NSCLC and Molm-14 AML cell lines. UNC-2025 blocks MERTK oncogenic signaling downstream in H2228 and H1299 cell lines, including basal and stimulated pAKT and pERK1/2. Additionally, UNC-2025 inhibits colony formation and triggers apoptotic cell death in four NSCLC cell lines.
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| Animal Protocol |
NOD/SCID/gamma mice
3 mg/kg Oral gavage |
| References |
| Molecular Formula |
C28H40N6O
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|---|---|
| Molecular Weight |
476.66
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| Exact Mass |
476.3263599
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| CAS # |
1429881-91-3
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| Related CAS # |
UNC2025 hydrochloride;2070015-17-5
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| Appearance |
Solid
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| SMILES |
CCCCNC1=NC=C2C(=CN(C2=N1)C3CCC(CC3)O)C4=CC=C(C=C4)CN5CCN(CC5)C
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| InChi Key |
MJSHVHLADKXCML-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H40N6O/c1-3-4-13-29-28-30-18-25-26(20-34(27(25)31-28)23-9-11-24(35)12-10-23)22-7-5-21(6-8-22)19-33-16-14-32(2)15-17-33/h5-8,18,20,23-24,35H,3-4,9-17,19H2,1-2H3,(H,29,30,31)
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| Chemical Name |
4-[2-(butylamino)-5-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]pyrrolo[2,3-d]pyrimidin-7-yl]cyclohexan-1-ol
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| Synonyms |
UNC2025; UNC 2025; UNC2025
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0979 mL | 10.4897 mL | 20.9793 mL | |
| 5 mM | 0.4196 mL | 2.0979 mL | 4.1959 mL | |
| 10 mM | 0.2098 mL | 1.0490 mL | 2.0979 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
UNC2025 inhibits colony formation in soft agar. Mol Cancer Ther. 2015 Sep;14(9):2014-22. |
UNC2025 Inhibits NSCLC tumor growth in vivo: H2228 (A) or A549 (B,C). Mol Cancer Ther. 2015 Sep; 14(9): 2014–2022. |
UNC2025 inhibits NSCLC tumor growth in vivo. Mol Cancer Ther. 2015 Sep;14(9):2014-22. |
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