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H3B-8800

Names

[ CAS No. ]:
1825302-42-8

[ Name ]:
H3B-8800

[Synonym ]:
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
(2S,3S,4E,6S,7R,10R)-7,10-Dihydroxy-3,7-dimethyl-12-oxo-2-[(2E,4E,6R)-6-(2-pyridinyl)-2,4-heptadien-2-yl]oxacyclododec-4-en-6-yl 4-methyl-1-piperazinecarboxylate

Biological Activity

[Description]:

H3B-8800 is an orally available splicing modulator that targets spliceosome SF3b complex containing either WTor mutant SF3B1 (binding IC50 of 0.3-2 nM); demonstrates dose-dependent inhibition of both canonical splicing and aberrant splicing induced by mutant SF3B1 in in vitro assays of biochemical splicing, induces lethality in spliceosome-mutant cancer cells. Blood Cancer Phase 1 Clinical

[References]

References 1. Seiler M, et al. Nat Med. 2018 Feb 19. doi: 10.1038/nm.4493. 2. Finci LI, et al. Genes Dev. 2018 Feb 1;32(3-4):309-320. 3. Cancer Discov. 2018 Mar 2. doi: 10.1158/2159-8290.CD-RW2018-038. View Related Products by Target Spliceosome Blood Cancer

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
710.6±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C31H45N3O6

[ Molecular Weight ]:
555.706

[ Flash Point ]:
383.6±32.9 °C

[ Exact Mass ]:
555.330811

[ LogP ]:
2.22

[ Vapour Pressure ]:
0.0±2.4 mmHg at 25°C

[ Index of Refraction ]:
1.581

Related Compounds