| Identification | Back Directory | [Name]
N-((4,5-difluoro-1H-benzo[d]imidazol-2-yl)methyl)-9-(3-fluorophenyl)-2-morpholino-9H-purin-6-amine | [CAS]
1454585-06-8 | [Synonyms]
SR-3029
CS-2390
SR-3029, >98%
SR-3029 (SR 3029
N-((4,5-difluoro-1H-benzo[d]imidazol-2-yl)methyl)-9-(3-fluorophenyl)-2-morpholino-9H-purin-6-amine
N-((6,7-Difluoro-1H-benzo[d]imidazol-2-yl)methyl)-9-(3-fluorophenyl)-2-morpholino-9H-purin-6-amine
N-[(6,7-Difluoro-1H-benzimidazol-2-yl)methyl]-9-(3-fluorophenyl)-2-(4-morpholinyl)-9H-purin-6-amine
9H-Purin-6-amine, N-[(6,7-difluoro-1H-benzimidazol-2-yl)methyl]-9-(3-fluorophenyl)-2-(4-morpholinyl)- | [Molecular Formula]
C23H19F3N8O | [MOL File]
1454585-06-8.mol | [Molecular Weight]
480.45 |
| Chemical Properties | Back Directory | [Boiling point ]
818.7±75.0 °C(Predicted) | [density ]
1.62±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30 mg/ml; DMSO: 30 mg/ml | [form ]
A solid | [pka]
8.76±0.30(Predicted) | [color ]
White to pink |
| Hazard Information | Back Directory | [Uses]
SR-3029 is a potent and selective CK1δ and CK1ε inhibitor (IC50 values are 44 and 260 nM, respectively). Exhibits selectivity for CK1δ and CK1ε over a panel of other kinases. Inhibits proliferation of melanoma and breast cancer cell lines in vitro. Also inhibits growth of breast tumor xenografts in mice. | [in vivo]
SR-3029 (20 mg/kg daily i.p.) exibits anti-tumor effects in rthotopic MDA-MB-231, MDA-MB-468 (TNBC), SKBR3 and BT474 (HER2+) tumor xenografts with no overt toxicity in mice. SR-3029 (20 mg/kg daily i.p.) also effectively inhibits the growth of tumor in primary patient-derived xenograft (PDX) models. In addition, SR-3029 (20 mg/kg, i.p.) strongly reduces the expression of nuclear β-catenin in tumors of mice[2]. | [IC 50]
CKIδ: 44 nM (IC50); CDK6/cyclin D3: 427 nM (IC50); CDK6/cyclin D1: 428 nM (IC50); CDK4/cyclin D3: 368 nM (IC50); CDK4/cyclin D1: 576 nM (IC50); FLT3: 3000 nM (IC50) | [storage]
Store at -20°C |
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