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Cemadotin

Names

[ CAS No. ]:
159776-69-9

[ Name ]:
Cemadotin

[Synonym ]:
UNII-6SQ8M7ZSFV
N,N-Dimethyl-L-valyl-L-valyl-N-methyl-L-valyl-L-prolyl-N-benzyl-L-prolinamide
Cemadotin
N,N-dimethyl-L-valyl-L-valyl-N-methyl-L-valyl-L-prolyl-N-(phenylmethyl)-L-prolinamide
L-Prolinamide,N,N-dimethyl-L-valyl-L-valyl-N-methyl-L-valyl-L-prolyl-N-(phenylmethyl)

Biological Activity

[Description]:

Cemadotin (LU103793) is an analogue of Dolastatin 15 (HY-P1126) which is naturally occurring cytotoxic peptides. Cemadotin blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin can be used to research anticancer[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin
Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

[Target]

Ki: 1 μM (tubulin)[1]


[In Vitro]

Cemadotin (0-100 μM; 35 min) inhibits polymerization dose-dependently in Tubulin-treated Strongylocentrotus purpuratus[1]. Cemadotin (0-1000 nM) preferentially suppresses the rate and extent of growing excursions of tubulin, and suppression is dependent upon the drug concentration[1]. Cemadotin (0-1 μM) markedly increases the rescue frequency but had little effect on the catastrophe frequency[1]. Cemadotin (400 pM~300 nM; 72 h) inhibits cancer cells HEK 293, F9 and HL60[2]. Cell Proliferation Assay[2] Cell Line: HEK 293, F9 and HL60 Concentration: 400 pM~300 nM Incubation Time: 72 h Result: Exhibited cytotoxicity against HEK 293, F9 and HL60 with IC50s of 0.7 nM, 14.8 nM and 0.5 nM, respectively.

Chemical & Physical Properties

[ Density]:
1.138g/cm3

[ Boiling Point ]:
857.7ºC at 760mmHg

[ Molecular Formula ]:
C35H56N6O5

[ Molecular Weight ]:
640.85600

[ Flash Point ]:
472.5ºC

[ Exact Mass ]:
640.43100

[ PSA ]:
122.37000

[ LogP ]:
3.15240

[ Vapour Pressure ]:
0mmHg at 25°C

[ Index of Refraction ]:
1.545

Related Compounds

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