An orally bioavailable inhibitor of Mer and Flt3
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UNC2025

Item No. 16613

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
trans-4-[2-(butylamino)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-cyclohexanol
CAS Number
1429881-91-3
Molecular Formula
C28H40N6O
Formula Weight
476.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 10 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:9): 0.1 mg/ml
λmax
222, 254, 290, 337 nm
SMILES
CCCCNC1=NC=C2C(N([C@@H]3CC[C@@H](O)CC3)C=C2C4=CC=C(CN5CCN(C)CC5)C=C4)=N1
InChi Code
InChI=1S/C28H40N6O/c1-3-4-13-29-28-30-18-25-26(20-34(27(25)31-28)23-9-11-24(35)12-10-23)22-7-5-21(6-8-22)19-33-16-14-32(2)15-17-33/h5-8,18,20,23-24,35H,3-4,9-17,19H2,1-2H3,(H,29,30,31)/t23-,24-
InChi Key
MJSHVHLADKXCML-RQNOJGIXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $83

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    10 mg

    $149

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    25 mg

    $351

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    50 mg

    $660

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    Product Description

    UNC2025 is a potent, orally bioavailable inhibitor of the tyrosine kinases Mer and Flt3 (IC50s = 0.74 and 0.80 nM, respectively).1 It less potently inhibits Axl and Tyro3 (IC50s = 14 and 17 nM, respectively) and a panel of related kinases.1 UNC2025 blocks colony formation of Mer- and Flt3-dependent tumor cell lines and inhibits Mer phosphorylation in bone marrow leukemia cells in vivo.1 Pharmacokinetic studies suggest that orally administered UNC2025 at 3 mg/kg will suffice to provide 90% inhibition of Mer and Flt3 at 30 min.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, W., DeRychere, D., Hunter, D., et al. UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor. J. Med. Chem. 57(16), 7031-7041 (2014).