| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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Purity: ≥98%
| Targets |
Mer (IC50 = 2.9 nM); Axl (IC50 = 37 nM); Tyro3 (IC50 = 48 nM); Mer (Ki = 4.3 nM)
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| ln Vitro |
In all cell lines, UNC569 (24 hours) elevated short-term PARP[2] and Caspase 3 levels as well as cellular fluorescence. Potent suppression of activated Mer and downstream signaling, including PI3K, is processed by UNC569 (1 μM; 1.5 hr). In human B-ALL (acute lymphoblastic leukemia) 697 and Jurkat cell lines, UNC569 (1 hr) inhibits Mer phosphorylation levels with IC50 values of 141 nM and 193 nM [1].
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| ln Vivo |
The pharmacokinetic characteristics of UNC569 (3 mg/kg) in vivo were assessed via in vitro (IV) and intravenous (PO) methods. Low systemic clearance (19.5 mL/min/kg), good wound bioavailability (57%) and high vial distribution (Vss of 5.83 L/kg) are characteristics of UNC569 [1]. For two weeks, bleached zebrafish were immersed in 4 μM UNC569. Comparing UNC569 to vehicle- and mock-treated fish, the results demonstrated a more than 50% reduction in tumor burden [2].
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| Cell Assay |
Apoptosis analysis [2]
Cell Types: 697 and Jurkat cells Tested Concentrations: 0.4μM, 0.8μM, 1μM, 1.2μM, 1.4μM, 1.6μM, 1.8μM, 2μM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of apoptosis. in all cell lines. Western Blot Analysis[2] Cell Types: 697 and Jurkat cells Tested Concentrations: 1 µM Incubation Duration: 1.5 hrs (hours) Experimental Results: Inhibition of Mer activation and downstream signaling through ERK1/2 and AKT. |
| References |
[1]. Jing Liu, et al. Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia. ACS Med Chem Lett. 2012 Feb 9;3(2):129-134.
[2]. Sandra Christoph, et al. UNC569, a novel small-molecule mer inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo. Mol Cancer Ther. 2013 Nov;12(11):2367-77. |
| Molecular Formula |
C22H29FN6
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|---|---|
| Molecular Weight |
396.504267454147
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| Exact Mass |
396.24
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| Elemental Analysis |
C, 66.64; H, 7.37; F, 4.79; N, 21.20
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| CAS # |
1350547-65-7
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| Related CAS # |
1350547-65-7
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| Appearance |
Solid powder
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| SMILES |
CCCCNC1=NC=C2C(=NN(C2=N1)CC3CCC(CC3)N)C4=CC=C(C=C4)F
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| InChi Key |
OGEBRHQLRGFBNV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H29FN6/c1-2-3-12-25-22-26-13-19-20(16-6-8-17(23)9-7-16)28-29(21(19)27-22)14-15-4-10-18(24)11-5-15/h6-9,13,15,18H,2-5,10-12,14,24H2,1H3,(H,25,26,27)
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| Chemical Name |
1-(((1r,4r)-4-aminocyclohexyl)methyl)-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine
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| Synonyms |
UNC569; UNC-569; UNC 569
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| HS Tariff Code |
2934.99.9001
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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) |
DMSO: ~31.3 mg/mL (~78.8 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.31 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5221 mL | 12.6103 mL | 25.2207 mL | |
| 5 mM | 0.5044 mL | 2.5221 mL | 5.0441 mL | |
| 10 mM | 0.2522 mL | 1.2610 mL | 2.5221 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.
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