ChemicalBook > CAS DataBase List > H3B-8800
(H3B8800)
H3B-8800 (H3B8800)
- Product Name
- H3B-8800 (H3B8800)
- CAS No.
- 1825302-42-8
- Chemical Name
- H3B-8800 (H3B8800)
- Synonyms
- H3B-8800 (RVT 2001);H3B-8800 (H3B8800);(2S,3S,6S,7R,10R,E)-7,10-Dihydroxy-3,7-dimethyl-12-oxo-2-((R,2E,4E)-6-(pyridin-2-yl)hepta-2,4-dien-2-yl)oxacyclododec-4-en-6-yl 4-methylpiperazine-1-carboxylate;1-Piperazinecarboxylic acid, 4-methyl-, (2S,3S,4E,6S,7R,10R)-7,10-dihydroxy-3,7-dimethyl-2-[(1E,3E,5R)-1-methyl-5-(2-pyridinyl)-1,3-hexadien-1-yl]-12-oxooxacyclododec-4-en-6-yl ester
- CBNumber
- CB14844852
- Molecular Formula
- C31H45N3O6
- Formula Weight
- 555.71
- MOL File
- 1825302-42-8.mol
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H3B-8800 (H3B8800) Property
- Boiling point:
- 710.6±60.0 °C(Predicted)
- Density
- 1.19±0.1 g/cm3(Predicted)
- solubility
- DMSO: Slightly soluble: 0.1-1 mg/ml
Ethanol: Slightly soluble: 0.1-1 mg/ml - form
- Solid
- pka
- 13.92±0.70(Predicted)
- color
- Yellow to orange
- InChIKey
- YOIQWBAHJZGRFW-WVRLKXNASA-N
- SMILES
- N1(C(O[C@@H]2[C@@](O)(C)CC[C@@H](O)CC(=O)O[C@H](/C(/C)=C/C=C/[C@H](C3=NC=CC=C3)C)[C@@H](C)C=C2)=O)CCN(C)CC1 |t:32|
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H3B-8800 (H3B8800) Chemical Properties,Usage,Production
Uses
H3B-8800 is a potent and orally active SF3B splicing modulator. H3B-8800 direct interaction with the SF3b complex and shows anti-cancer activity. H3B-8800 has the potential for the research of acute myeloid leukemia (AML) with SF3B1 mutant[1].
in vivo
H3B-8800 (2, 4 mg/kg; p.o.; daily) shows anti tumor activity in AML derived xenografts (PDXs) with a mutation in SF3B1[1].
| Animal Model: | 6-8 weeks, female NSG or CB17-SCID mice (K562 cells with SF3B1WT or SF3B1K700E)[1] |
| Dosage: | 2, 4 mg/kg |
| Administration: | P.o.; daily |
| Result: | Resulted in antileukemic efficacy and splicing modulation in mice bearing AML patient-derived xenografts (PDXs) with a mutation in SF3B1 but had little effect in mice bearing SF3B1WT AML PDXs, significantly reduced leukemic burden relative in SF3B1K700E PDX. |
References
[1] Seiler M, et al. H3B-8800, an orally available small-molecule splicing modulator, induces lethality in spliceosome-mutant cancers. Nat Med. 2018 May;24(4):497-504. DOI:10.1038/nm.4493
H3B-8800 (H3B8800) Preparation Products And Raw materials
Raw materials
Preparation Products
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