A GPR132 agonist
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Product Type

Small Molecule Modulators
Receptor Pharmacology
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Research Area

Cancer

ONC212

Item No. 30931

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,4,6,7,8,9-hexahydro-7-(phenylmethyl)-4-[[4-(trifluoromethyl)phenyl]methyl]-imidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one
CAS Number
1807861-48-8
Molecular Formula
C24H23F3N4O
Formula Weight
440.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
232 nm
SMILES
O=C(N(CC1=CC=C(C(F)(F)F)C=C1)C2=NCCN23)C4=C3CCN(C4)CC5=CC=CC=C5
InChi Code
InChI=1S/C24H23F3N4O/c25-24(26,27)19-8-6-18(7-9-19)15-31-22(32)20-16-29(14-17-4-2-1-3-5-17)12-10-21(20)30-13-11-28-23(30)31/h1-9H,10-16H2
InChi Key
DFULPGUTXZTYKA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    ONC212 is an agonist of the orphan G protein-coupled receptor GPR132 (EC50 = ~400 nM in a PathHunter® β-arrestin assay).1 It inhibits cell growth in a panel of 62 human leukemia cell lines, including acute myeloid leukemia (AML), acute lymphoblastic leukemia (ALL), chronic myelogenous leukemia (CML), and hairy cell leukemias, with GI50 values ranging from less than 78 to 456 nM. ONC212 also reduces cell growth in a panel of 58 lymphoma cell lines (GI50s = <78-261 nM). In vivo, ONC212 (50 mg/kg) reduces tumor volume in HT-29 and HCT116 mouse xenograft models.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Prabhu, V.V., Madhukar, N., Tarapore, R., et al. Abstract 1155: Potent anti-cancer effects of selective GPR132/G2A agonist imipridone ONC212 in leukemia and lymphoma. Cancer Res. 77(13), (2017).

    2. Wagner, J., Kline, C.L., Ralff, M.D., et al. Preclinical evaluation of the imipridone family, analogs of clinical stage anti-cancer small molecule ONC201, reveals potent anti-cancer effects of ONC212. Cell Cycle 16(19), 1790-1799 (2017).