A pan PKD inhibitor
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CRT0066101 (hydrochloride)

Item No. 15337

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)-phenol, trihydrochloride
CAS Number
1781742-22-0
Molecular Formula
C18H22N6O • 3HCl
Formula Weight
447.8
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.1 mg/mlDMSO: 3 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlWater: 10 mg/ml
λmax
250 nm
SMILES
N[C@H](CC)CNC1=CC=NC(C2=C(O)C=CC(C3=CN(C)N=C3)=C2)=N1.Cl.Cl.Cl
InChi Code
InChI=1S/C18H22N6O.3ClH/c1-3-14(19)10-21-17-6-7-20-18(23-17)15-8-12(4-5-16(15)25)13-9-22-24(2)11-13;;;/h4-9,11,14,25H,3,10,19H2,1-2H3,(H,20,21,23);3*1H/t14-;;;/m1.../s1
InChi Key
HWZPJKPBOZVLEB-XJCLVHIMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $38

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    5 mg

    $110

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    10 mg

    $202

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    Product Description

    CRT0066101 is an inhibitor of all three PKD isoforms (IC50s = 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively).1 It exhibits selectivity for PKD against a panel of >90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl.1 It can block cell proliferation, induce apoptosis, and reduce the viability of pancreatic cancer cells both in vitro and in vivo.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Harikumar, K.B., Kunnumakkara, A.B., Ochi, N., et al. A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo. Mol. Cancer Ther. 9(5), 1136-1146 (2010).