A TAM family kinase inhibitor
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UNC569

Item No. 22966

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[(trans-4-aminocyclohexyl)methyl]-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine
CAS Number
1350547-65-7
Molecular Formula
C22H29FN6
Formula Weight
396.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2.5 mg/mlDMF:PBS (pH 7.2) (1:4): 0.2 mg/mlDMSO: 0.2 mg/mlEthanol: 2 mg/ml
λmax
246, 308 nm
SMILES
CCCCNC1=NC=C2C(N(C[C@H]3CC[C@H](N)CC3)N=C2C4=CC=C(F)C=C4)=N1
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-
InChi Key
OGEBRHQLRGFBNV-RZDIXWSQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $157

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    10 mg

    $293

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    25 mg

    $631

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    Product Description

    UNC569 is a potent inhibitor of the TAM family receptor tyrosine kinases Mer, Axl, and Tyro3 (IC50s = 2.9, 37, and 48 nM, respectively).1 It has antiproliferative activity in vitro against acute lymphoblastic leukemia (ALL) cells (IC50s = 0.5 and 1.2 μM for 697 and Jurkat cell lines, respectively) and inhibits Mer phosphorylation (IC50s = 141 and 193 nM in 697 and Jurkat cell lines, respectively). UNC569 activates Akt and ERK1/2 phosphorylation, induces apoptosis, and sensitizes ALL cells to etoposide (Item No. 12092) and methotrexate (Item No. 13960). In vivo, UNC569 (4 μM) decreases tumor burden by 47.8% relative to vehicle controls in human MYC transgenic zebrafish. UNC569 (10 mg/kg) delays leukemia onset, reduces CNS infiltration, and prolongs survival of mice implanted with patient-derived Mer-expressing ALL primary cells.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Christoph, S., DeRyckere, D., Schlegel, J., et al. UNC569, a novel small-molecule mer inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo. Mol. Cancer Ther. 12(11), 2367-2377 (2013).

    2. Krause, S., Pfeiffer, C.M., Strube, S., et al. Mer tyrosine kinase promotes the survival of t(1;19)-positive acute lymphoblastic leukemia (ALL) in the central nervous system (CNS). Blood 125(5), 820-830 (2015).