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Cytotoxic Agents

What is Pyrrolobenzodiazepine (PBD)?

Structure of Pyrrolobenzodiazepine Pyrrolobenzodiazepine (PBD) Chemical Name: Diazepinoindole; Molecular Formula: C14H14N2O3 Molecular weight 258,27 g/mole Average mass: 181.193 Da Monoisotopic mass: 181.063995 Da Pyrrolobenzodiazepine (PBDs) are a class of sequence-selective...

What is Monomethyl Auristatin F (MMAF)?

Monomethyl Auristatin F Chemical Name: (S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-N,3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoic acid Molecular Weight: 731.96 Formula: C39H65N5O8 CAS#: 141205-32-5 Solubility: DMSO up to 20 mM Biological Activity Monomethyl auristatin F (MMAF) is an antitubulin agent agent that...

What is Monomethyl Auristatin E (MMAE)?

Monomethyl Auristatin E Chemical Name: (S)-N-((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1S,2R)-1-hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxoheptan-4-yl)-N,3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamide Molecular Weight: 717.98 Formula: C39H67N5O7 CAS: 474645-27-7 Solubility: DMSO up to 20 mM Biological Activity Monomethyl auristatin E (MMAE, vedotin) is a very potent antimitotic agent...

What is Maytansine?

Maytansine Chemical Name: L-alanine, N-acetyl-N-methyl-, 11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclohexacosa-10,12,14(26),16,18-pentaen-6-yl ester, Molecular Weight: 692.19614 Formula: C34H46ClN3O10 CAS#: 35846-53-8 Biological Activity Maytansine, a benzoansamacrolide, is a highly potent microtubule-targeted compound that induces...

What are Duocarmycin analogues?

Duocarmycin A Chemical Name: 1,2,4,5,8,8a-hexahydro-4-oxo-2--cyclopropapyrroloindole-6-carboxylic acid methyl ester, (+)-duocarmycin SA, duocarmycin SA, antibiotic DC 113 Molecular Weight: 477.47 Formula: C25H23N3O7 CAS#: 130288-24-3 Solubility: Sparingly Soluble (0.030 g/L) (25 ºC),...

What is Dolastatins (Dolastatin 10 and Dolastatin 15)?

Structure of Dolastatin 10 Dolastatin 10 Systematic name: N,N-Dimethyl-L-valyl-N-amino}propyl]-1-pyrrolidinyl}-5-methyl-1-oxo-4-heptanyl]-N-methyl-L -valinamide Molecular Formula: C42H68N6O6S Molecular weight 785.09092 g/mol Average mass: 785.091 Da Monoisotopic mass: 784.492126 Da Structure of Dolastatin 15 Dolastatin...

What is Centanamycin (ML-970; Indolecarboxamide)?

Chemical name: N--5,6,7-trimethoxy-1H-indole-2-carboxamide Centanamycin, also known as  ML-970, AS-I-145 and NSC 716970, is an indolecarboxamide synthesized as a less toxic analog...

Calicheamicin and DNA-cleaving

Calicheamicins, isolated from Micromonospora echinospora ssp. calichensis, combine unprecedented and extraordinary chemical and biological properties.  This includes activity in the biochemical...
Calicheamicin

What is Calicheamicin?

Calicheamicin (also known as LL-E33288 antibiotics) was first discovered in the mid-1980s by a scientist from American Cyanamid Company’s medical research division, Lederle...

Cytotoxic Agents and Antibody-drug Conjugates

Drug name  Target  Mode of Action  Example Auristatins α-Tubulin Prevent tubulin polymerization Monomethyl Auristatin E (MMAE) Monomethyl Auristatin F (MMAF) Maytansinoids α-Tubulin Prevent tubulin polymerization Calicheamicins Sequence-specific minor groove of...

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