UNC569

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.

Product information

CAS Number: 1350547-65-7

Molecular Weight: 396.50

Formula: C22H29FN6

Synonym:

UNC 569

UNC569

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

Smiles: CCCCNC1=NC=C2C(=N1)N(C[C@@H]1CC[C@@H](N)CC1)N=C2C1=CC=C(F)C=C1

InChiKey: OGEBRHQLRGFBNV-RZDIXWSQSA-N

InChi: 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-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

References:

1. 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. PubMed PMID: 23997116; PubMed Central PMCID: PMC3823742.

Products are for research use only. Not for human use.