| Identification | Back Directory | [Name]
1H-Cyclopenta[b]benzofuran-2-carboxamide, 2,3,3a,8b-tetrahydro-1,8b-dihydroxy-N,6,8-trimethoxy-3a-(4-methoxyphenyl)-N-methyl-3-phenyl-, (1R,2R,3S,3aR,8bS)- | [CAS]
1139253-73-8 | [Synonyms]
1H-Cyclopenta[b]benzofuran-2-carboxamide, 2,3,3a,8b-tetrahydro-1,8b-dihydroxy-N,6,8-trimethoxy-3a-(4-methoxyphenyl)-N-methyl-3-phenyl-, (1R,2R,3S,3aR,8bS)- | [Molecular Formula]
C29H31NO8 | [MOL File]
1139253-73-8.mol | [Molecular Weight]
521.56 |
| Chemical Properties | Back Directory | [Boiling point ]
646.3±65.0 °C(Predicted) | [density ]
1.340±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
11.63±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
Rohinitib is a HSF1 inhibitor for target-based cancer therapy. | [Uses]
Rohinitib is a potent and specific eIF4A inhibitor. Rohinitib induces cell apoptosis of acute myeloid leukemia (AML) cell lines and reduces the leukemia burden of AML xenograft model. Rohinitib can be used for the research of AML[1]. | [in vivo]
Rohinitib (0.75 and 1.0 mg/kg; s.c. once daily for 5 consecutive days until mice get moribund) shows anti-AML effects in vivo[1]. | Animal Model: | Female NSG mice with AML xenografts generated by intravenous injections of MOLM-13 cells[1] | | Dosage: | 0.75 and 1.0 mg/kg | | Administration: | Subcutaneous injection; 0.75 and 1.0 mg/kg once daily 5 days a week until mice get moribund | | Result: | Significantly reduced the leukemia burden, circulating and BM leukemic human CD45+ cells. Dose-dependently prolonged the survival rate of mice.
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| [References]
[1] Nishida Y, et alJ. Inhibition of translation initiation factor eIF4a inactivates heat shock factor 1 (HSF1) and exerts anti-leukemia activity in AML. Leukemia. 2021 Sep;35(9):2469-2481. DOI:10.1038/s41375-021-01308-z |
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