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UNC 569 hydrochloride

Catalog No. T21302L

Synonyms: UNC 569 hydrochloride (1350547-65-7 Free base)

UNC 569 hydrochloride is a reversible and ATP-competitive inhibitor of Mer with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC 569 hydrochloride inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC 569 hydrochloride can be used in studies about acute lymphoblastic leukemia and atypical teratoid/rhabdoid tumors.

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UNC 569 hydrochloride, CAS N/A

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	UNC 569 hydrochloride is a reversible and ATP-competitive inhibitor of Mer with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC 569 hydrochloride inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC 569 hydrochloride can be used in studies about acute lymphoblastic leukemia and atypical teratoid/rhabdoid tumors.
In vitro	UNC 569 hydrochloride inhibits Mer phosphorylation levels with IC50 values of 141 nM and 193 nM in human B-ALL 697 and Jurkat cell lines, respectively. UNC 569 hydrochloride (1 µM) treatment effectively inhibits the activation of Mer and downstream signaling, including the PI3K/AKT and MAPK/ERK pathways. In ALL cell lines, UNC 569 hydrochloride (0.4 -2 µM) induces apoptosis and increases the levels of cleaved Caspase 3 and cleaved PARP[1].
In vivo	In Leukemic zebrafish, UNC 569 hydrochloride (4 µM) induces more than 50% reduction in tumor burden compared with vehicle- and mock-treated fish[1]. UNC 569 hydrochloride has low systemic clearance (19.5 mL/min/kg), high volume of distribution (Vss of 5.83 L/kg), and good oral bioavailability (57%)[2].

Synonyms	UNC 569 hydrochloride (1350547-65-7 Free base)
Molecular Weight	432.96
Formula	C22H30ClFN6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. 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. 2. 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.

Related Products

Related compounds with same targets

DS-1205 ONO-7475 2-D08 NPS-1034 Pralatrexate S49076 HCl S49076 UNC 569 hydrochloride

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Keywords

UNC 569 hydrochloride Tyrosine Kinase/Adaptors TAM Receptor UNC 569 hydrochloride (1350547-65-7 Free base) Inhibitor inhibitor inhibit

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