1825302-42-8

1825302-42-8 structure

Name: H3B-8800
Chemical Name: (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
CAS Number: 1825302-42-8
Molecular Formula: C₃₁H₄₅N₃O₆
Molecular Weight: 555.706
Create Date: 2020-01-17 10:23:22
Modify Date: 2024-01-04 15:07:38
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

Name	(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
Synonyms	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

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