| Identification | Back Directory | [Name]
Imidazo[1,2-c]pyrimidine-2-carbonitrile, 8-[4-[(dimethylamino)methyl]-2-methylphenyl]-5-[[(5-fluoro-2,3-dihydro-4-benzofuranyl)methyl]amino]- | [CAS]
2369769-29-7 | [Synonyms]
ORIC-944
Imidazo[1,2-c]pyrimidine-2-carbonitrile, 8-[4-[(dimethylamino)methyl]-2-methylphenyl]-5-[[(5-fluoro-2,3-dihydro-4-benzofuranyl)methyl]amino]- | [Molecular Formula]
C26H25FN6O | [MOL File]
2369769-29-7.mol | [Molecular Weight]
456.51 |
| Chemical Properties | Back Directory | [density ]
1.31±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
8.73±0.28(Predicted) | [color ]
White to off-white | [InChIKey]
FLCIOLFIDGTRCI-UHFFFAOYSA-N | [SMILES]
C1(NCC2=C3C(=CC=C2F)OCC3)=NC=C(C2=CC=C(CN(C)C)C=C2C)C2=NC(C#N)=CN12 |
| Hazard Information | Back Directory | [Uses]
ORIC-944 is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer. | [in vivo]
ORIC-944 (30, 100, 200 mg/kg; op; everyday for 50 days) induces significantly tumor regressions at all dose levels
tested[3].
ORIC-944 (30 mg/kg; op; everyday for 30 days) demonstrates strong single agent activity to enzalutamide in prostate cancer xenograft model[3]. | Animal Model: | KARPAS-422 DLBCL xenograft model[1] | | Dosage: | 30, 100, 200 mg/kg | | Administration: | Oral gavage (p.o.) | | Result: | Had well tolerated at all dose
levels assessed compared to tazemetostat at a clinically relevant dose. |
| Animal Model: | 22Rv1 model | | Dosage: | 30 mg/kg | | Administration: | Oral gavage (p.o.) | | Result: | Made average tumor volume ± SEM, with n=8-10/group.
Had a significant difference in ORIC-944 treatment group vs vehicle. |
| [References]
[1] Daemen A, et al. ORIC-944, a potent and selective allosteric PRC2 inhibitor with best-in-class properties, demonstrates combination synergy with AR pathway inhibitors in prostate cancer models[J]. Cancer Research, 2024, 84(6_Supplement): 6586-6586.
[2] ORIC Pharmaceuticals Provides Initial Phase 1b Data for ORIC-944, Operational Highlights for 2023, and Anticipated Upcoming Milestones |
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