UNC569 | CAS#1350547-65-7 | MER Inhbitor

MedKoo Cat#: 406553 | Name: UNC569

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

UNC569 is a novel small-molecule MER inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo. UNC569 is the first small-molecule Mer inhibitor. UNC569 inhibited Mer activation and downstream signaling through ERK1/2 and AKT. Treatment with UNC569 reduced proliferation/survival in liquid culture, decreased colony formation in methylcellulose/soft agar, and increased sensitivity to cytotoxic chemotherapies. Mer receptor tyrosine kinase is ectopically expressed in ALL patient samples and cell lines.

Chemical Structure

UNC569

CAS#1350547-65-7

Theoretical Analysis

MedKoo Cat#: 406553

Name: UNC569

CAS#: 1350547-65-7

Chemical Formula: C22H29FN6

Exact Mass: 396.2438

Molecular Weight: 396.50

Elemental Analysis: C, 66.64; H, 7.37; F, 4.79; N, 21.20

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 450.00	2 Weeks
25mg	USD 900.00

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Related CAS #

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Synonym

UNC569, UNC569, UNC 569

IUPAC/Chemical Name

1-(((1r,4r)-4-aminocyclohexyl)methyl)-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine

InChi Key

OGEBRHQLRGFBNV-RZDIXWSQSA-N

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)/t15-,18-

SMILES Code

FC1=CC=C(C2=NN(C[C@H]3CC[C@H](N)CC3)C4=NC(NCCCC)=NC=C42)C=C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 396.50 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Yan L, Chen C, Wang L, Hong H, Wu C, Huang J, Jiang J, Chen J, Xu G, Cui Z. Analysis of gene expression in microglial apoptotic cell clearance following spinal cord injury based on machine learning algorithms. Exp Ther Med. 2024 May 22;28(1):292. doi: 10.3892/etm.2024.12581. PMID: 38827468; PMCID: PMC11140288. 2: Pastore M, Caligiuri A, Raggi C, Navari N, Piombanti B, Di Maira G, Rovida E, Piccinni MP, Lombardelli L, Logiodice F, Rombouts K, Petta S, Marra F. Macrophage MerTK promotes profibrogenic cross-talk with hepatic stellate cells via soluble mediators. JHEP Rep. 2022 Feb 1;4(4):100444. doi: 10.1016/j.jhepr.2022.100444. PMID: 35252828; PMCID: PMC8891698. 3: Xie X, Li M, Feng B, Li J, Sun Z, Zhao Y, Lu C. The Cellular Mechanisms of Dopamine Modulation on the Neuronal Network Oscillations in the CA3 Area of Rat Hippocampal Slices. Neuroscience. 2021 Nov 1;475:83-92. doi: 10.1016/j.neuroscience.2021.09.005. Epub 2021 Sep 14. PMID: 34534635. 4: Sayama A, Okado K, Yamaguchi M, Samata N, Imaoka M, Kai K, Mori K. The Impact of the Timing of Dosing on the Severity of UNC569-Induced Ultrastructural Changes in the Mouse Retina. Toxicol Pathol. 2020 Jul;48(5):669-676. doi: 10.1177/0192623320931415. Epub 2020 Jun 15. PMID: 32538308. 5: Sayama A, Okado K, Nakamura K, Kawaguchi T, Iguchi T, Makino T, Yabe K, Kai K, Mori K. UNC569-induced Morphological Changes in Pigment Epithelia and Photoreceptor Cells in the Retina through MerTK Inhibition in Mice. Toxicol Pathol. 2018 Feb;46(2):193-201. doi: 10.1177/0192623317749469. Epub 2018 Jan 8. PMID: 29310530. 6: Koda Y, Itoh M, Tohda S. Effects of MERTK Inhibitors UNC569 and UNC1062 on the Growth of Acute Myeloid Leukaemia Cells. Anticancer Res. 2018 Jan;38(1):199-204. doi: 10.21873/anticanres.12208. PMID: 29277773. 7: Nomura K, Vilalta A, Allendorf DH, Hornik TC, Brown GC. Activated Microglia Desialylate and Phagocytose Cells via Neuraminidase, Galectin-3, and Mer Tyrosine Kinase. J Immunol. 2017 Jun 15;198(12):4792-4801. doi: 10.4049/jimmunol.1502532. Epub 2017 May 12. PMID: 28500071; PMCID: PMC5458330. 8: Bernsmeier C, Pop OT, Singanayagam A, Triantafyllou E, Patel VC, Weston CJ, Curbishley S, Sadiq F, Vergis N, Khamri W, Bernal W, Auzinger G, Heneghan M, Ma Y, Jassem W, Heaton ND, Adams DH, Quaglia A, Thursz MR, Wendon J, Antoniades CG. Patients with acute-on-chronic liver failure have increased numbers of regulatory immune cells expressing the receptor tyrosine kinase MERTK. Gastroenterology. 2015 Mar;148(3):603-615.e14. doi: 10.1053/j.gastro.2014.11.045. Epub 2014 Dec 3. PMID: 25479139. 9: Krause S, Pfeiffer C, Strube S, Alsadeq A, Fedders H, Vokuhl C, Loges S, Waizenegger J, Ben-Batalla I, Cario G, Möricke A, Stanulla M, Schrappe M, Schewe DM. Mer tyrosine kinase promotes the survival of t(1;19)-positive acute lymphoblastic leukemia (ALL) in the central nervous system (CNS). Blood. 2015 Jan 29;125(5):820-30. doi: 10.1182/blood-2014-06-583062. Epub 2014 Nov 26. PMID: 25428221. 10: Christoph S, Deryckere D, Schlegel J, Frazer JK, Batchelor LA, Trakhimets AY, Sather S, Hunter DM, Cummings CT, Liu J, Yang C, Kireev D, Simpson C, Norris-Drouin J, Hull-Ryde EA, Janzen WP, Johnson GL, Wang X, Frye SV, Earp HS 3rd, Graham DK. 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. doi: 10.1158/1535-7163.MCT-13-0040. Epub 2013 Aug 30. PMID: 23997116; PMCID: PMC3823742.