UNC2250 | CAS#1493694-70-4 | Mer Kinase Inhibitor

MedKoo Cat#: 406396 | Name: UNC2250

Description:

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

UNC2250 is a potent and selective Mer Kinase inhibitor. When applied to live cells, UNC2250 inhibited steady-state phosphorylation of endogenous Mer with an IC50 of 9.8 nM and blocked ligand-stimulated activation of a chimeric EGFR-Mer protein. Treatment with UNC2250 also resulted in decreased colony-forming potential in rhabdoid and NSCLC tumor cells, thereby demonstrating functional antitumor activity. The results provide a rationale for further investigation of UNC2250 for therapeutic application in patients with cancer.

Chemical Structure

UNC2250

CAS#1493694-70-4

Theoretical Analysis

MedKoo Cat#: 406396

Name: UNC2250

CAS#: 1493694-70-4

Chemical Formula: C24H36N6O2

Exact Mass: 440.2900

Molecular Weight: 440.58

Elemental Analysis: C, 65.43; H, 8.24; N, 19.07; O, 7.26

Price and Availability

Size	Price	Availability
10mg	USD 150.00	Ready to ship
25mg	USD 250.00	Ready to ship
50mg	USD 450.00	Ready to ship
100mg	USD 750.00	Ready to ship
200mg	USD 1,250.00	Ready to ship
500mg	USD 2,450.00	Ready to ship
1g	USD 3,450.00	2 weeks
2g	USD 5,850.00	2 weeks

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Related CAS #

No Data

Synonym

UNC2250, UNC-2250, UNC 2250

IUPAC/Chemical Name

(1r,4r)-4-((2-(butylamino)-5-(5-(morpholinomethyl)pyridin-2-yl)pyrimidin-4-yl)amino)cyclohexanol

InChi Key

HSYSSKFCQHXOBP-MXVIHJGJSA-N

InChi Code

InChI=1S/C24H36N6O2/c1-2-3-10-25-24-27-16-21(23(29-24)28-19-5-7-20(31)8-6-19)22-9-4-18(15-26-22)17-30-11-13-32-14-12-30/h4,9,15-16,19-20,31H,2-3,5-8,10-14,17H2,1H3,(H2,25,27,28,29)/t19-,20-

SMILES Code

O[C@H]1CC[C@H](NC2=NC(NCCCC)=NC=C2C3=NC=C(CN4CCOCC4)C=C3)CC1

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

Certificate of Analysis

View CoA: current batch, Lot#BBC60304

QC Data

View QC data: current batch, Lot#BBC60304

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 440.58 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: Chen F, Li Y, Zhao L, Lin C, Zhou Y, Ye W, Wan W, Zou H, Xue Y. Anti- inflammatory effects of MerTK by inducing M2 macrophage polarization via PI3K/Akt/GSK-3β pathway in gout. Int Immunopharmacol. 2024 Dec 5;142(Pt A):112942. doi: 10.1016/j.intimp.2024.112942. Epub 2024 Aug 31. PMID: 39217874. 2: Xu H, Qin X, Guo Y, Zhao S, Feng X, Zhang R, Tian T, Kong L, Yang C, Zhang Z. Radiation-based immunogenic vaccine combined with a macrophage "checkpoint inhibitor" for boosting innate and adaptive immunity against metastatic colon cancers. Acta Pharm Sin B. 2024 May;14(5):2247-2262. doi: 10.1016/j.apsb.2024.02.015. Epub 2024 Feb 27. PMID: 38799631; PMCID: PMC11120279. 3: Lee YJ, Park M, Kim HY, Kim JK, Kim WK, Lim SC, Kang KW. Circulating small extracellular vesicles promote proliferation and migration of vascular smooth muscle cells via AXL and MerTK activation. Acta Pharmacol Sin. 2023 May;44(5):984-998. doi: 10.1038/s41401-022-01029-8. Epub 2022 Nov 30. PMID: 36450791; PMCID: PMC10104856. 4: Fukatsu M, Ohkawara H, Wang X, Alkebsi L, Furukawa M, Mori H, Fukami M, Fukami SI, Sano T, Takahashi H, Harada-Shirado K, Kimura S, Sugimoto K, Ogawa K, Ikezoe T. The suppressive effects of Mer inhibition on inflammatory responses in the pathogenesis of LPS-induced ALI/ARDS. Sci Signal. 2022 Mar 8;15(724):eabd2533. doi: 10.1126/scisignal.abd2533. Epub 2022 Mar 8. PMID: 35258998. 5: Du Y, Lu Z, Yang D, Wang D, Jiang L, Shen Y, Du Q, Yu W. MerTK inhibits the activation of the NLRP3 inflammasome after subarachnoid hemorrhage by inducing autophagy. Brain Res. 2021 Sep 1;1766:147525. doi: 10.1016/j.brainres.2021.147525. Epub 2021 May 16. PMID: 34010608. 6: Hoque M, Wai Wong S, Recasens A, Abbassi R, Nguyen N, Zhang D, Stashko MA, Wang X, Frye S, Day BW, Baell J, Munoz L. MerTK activity is not necessary for the proliferation of glioblastoma stem cells. Biochem Pharmacol. 2021 Apr;186:114437. doi: 10.1016/j.bcp.2021.114437. Epub 2021 Feb 8. PMID: 33571503. 7: Furukawa M, Wang X, Ohkawara H, Fukatsu M, Alkebsi L, Takahashi H, Harada- Shirado K, Shichishima-Nakamura A, Kimura S, Ogawa K, Ikezoe T. A critical role of the Gas6-Mer axis in endothelial dysfunction contributing to TA-TMA associated with GVHD. Blood Adv. 2019 Jul 23;3(14):2128-2143. doi: 10.1182/bloodadvances.2019000222. PMID: 31300420; PMCID: PMC6650735. 8: Shi C, Li X, Wang X, Ding N, Ping L, Shi Y, Mi L, Lai Y, Song Y, Zhu J. The proto-oncogene Mer tyrosine kinase is a novel therapeutic target in mantle cell lymphoma. J Hematol Oncol. 2018 Mar 20;11(1):43. doi: 10.1186/s13045-018-0584-6. PMID: 29554921; PMCID: PMC5859520. 9: Zhang W, Zhang D, Stashko MA, DeRyckere D, Hunter D, Kireev D, Miley MJ, Cummings C, Lee M, Norris-Drouin J, Stewart WM, Sather S, Zhou Y, Kirkpatrick G, Machius M, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X. Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors. J Med Chem. 2013 Dec 12;56(23):9683-92. doi: 10.1021/jm401387j. Epub 2013 Nov 20. Erratum in: J Med Chem. 2014 Aug 28;57(16):7141. PMID: 24195762; PMCID: PMC3980660.