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123884-00-4

123884-00-4 structure
123884-00-4 structure
  • Name: Dolastatin 15
  • Chemical Name: Dolastatin 15
  • CAS Number: 123884-00-4
  • Molecular Formula: C45H68N6O9
  • Molecular Weight: 837.05600
  • Catalog: Signaling Pathways Antibody-drug Conjugate ADC Cytotoxin
  • Create Date: 2017-12-30 23:48:13
  • Modify Date: 2025-08-26 19:19:13
  • Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin[1][2][3].

Name Dolastatin 15
Synonyms (5S)-1-[(2S)-O-(N,N-DIMETHYL-VAL-VAL-N-ME-VAL-PRO-PRO)-2-HYDROXYISOVALERYL]-2-OXO-4-METHOXY-5-BENZYL-3-PYRROLINE
(5S)-1-[(2S)-O-(N,N-Val-Val-N-Me-Val-Pro-Pro)-2-hydroxyisovaleryl]-2-oxo-4-methoxy-5-benzyl-3-pyrroline
(5S)-1-{(2S)-O-[(N,N-dimethyl-L-valyl)-L-valyl-(N-methyl-L-valyl)-L-prolyl-L-prolyl]-2-hydroxy-isovaleryl}-2-oxo-4-methoxy-5-benzyl-3-pyrroline
(5S)-1-[N,N-Dimethyl-L-Val-L-Val-N-methyl-L-Val-L-Pro-L-Pro-L-Hyiv-]-5-benzyl-4-methoxy-1H-pyrrol-2(5H)-one
L-Proline,1-(1-(N-(N-(N,N-dimethyl-L-valyl)-L-valyl)-N-methyl-L-valyl)-L-propyl)-,1-((2,5-dihydro-3-methoxy-5-oxo-2-(phenylmethyl)-1H-pyrrol-1-yl)carbonyl)-2-methylpropyl ester,(S-(R*,R*))
dolastatin-15
L-Proline,1-(1-(N-(N-(N,N-dimethyl-L-valyl)-L-valyl)-N-methyl-L-valyl)-L-prolyl)-,1-((2,5-dihydro-3-methoxy-5-oxo-2-(phenylmethyl)-1H-pyrrol-1-yl)carbonyl)-2-methylpropyl ester,(S-(R*,R*))
Description Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin[1][2][3].
Related Catalog
Target

Auristatin

In Vitro Dolastatin 15 (DLS 15) induces cell cycle arrest at the G2/M phase followed by apoptosis in various human myeloma cell lines (RPMI8226, U266, and IM9). Dolastatin 15 induces apoptosis of myeloma cells via activation of both mitochondrial- and Fas (CD95)/Fas-L (CD95-L)-mediated pathways[2]. Dolastatin 15 (DLS 15) displays growth inhibitory activity against all four SCLC cell lines (NCI-H69, NCI-H82, NCI-H345, NCI-H446) with IC50 values ranging from 0.039-28.8 nM, which were 2.7-9.2-fold higher than the values for dolastatin 10. All four SCLC cell lines underwent G2/M arrest within 24 hours of exposure to dolastatin 15[4].
In Vivo Dolastatin 15 conjugates to Trastuzumab via lysine residues at the drug C-terminus using a non-cleavable linker (Trastuzumab-amide-C-term-Dol15) produced target-dependent growth inhibition of cells endogenously expressing high HER2 levels (i.e., SK-BR-3, SK-OV-3) in vitro. This ADC was effective at varying doses (i.e., 10 and 20 mg/kg) in the SK-OV-3 human ovarian cancer xenograft[3].
References

[1]. Bai R, et al. Dolastatin 15, a potent antimitotic depsipeptide derived from Dolabella auricularia. Interaction with tubulin and effects of cellular microtubules. Biochem Pharmacol. 1992 Jun 23;43(12):2637-45.

[2]. Sato M, et al. A natural peptide, dolastatin 15, induces G2/M cell cycle arrest and apoptosis of human multiple myeloma cells. Int J Oncol. 2007 Jun;30(6):1453-9.

[3]. Gianolio DA, et al. Targeting HER2-positive cancer with dolastatin 15 derivatives conjugated to trastuzumab, novel antibody-drug conjugates. Cancer Chemother Pharmacol. 2012 Sep;70(3):439-49.

[4]. Ali MA, et al. Dolastatin 15 induces apoptosis and BCL-2 phosphorylation in small cell lung cancer cell lines. Anticancer Res. 1998 Mar-Apr;18(2A):1021-6.

Density 1.2g/cm3
Boiling Point 943.2ºC at 760mmHg
Molecular Formula C45H68N6O9
Molecular Weight 837.05600
Flash Point 524.2ºC
Exact Mass 836.50500
PSA 166.18000
LogP 3.46120
Vapour Pressure 0mmHg at 25°C
Index of Refraction 1.572
Storage condition -20°C
Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR NONH for all modes of transport
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