| Identification | Back Directory | [Name]
CL2A-SN-38 | [CAS]
1279680-68-0 | [Synonyms]
CL2A-SN-38
[4-[[(2S)-2-(4-Aminobutyl)-35-[4-[[[[4-[(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)methyl]cyclohexyl]carbonyl]amino]methyl]-1H-1,2,3-triazol-1-yl]-1,4,8-trioxo-6,12,15,18,21,24,27,30,33-nonaoxa-3,9-diazapentatriacont-1-yl]amino]phenyl]methyl(4S)-4,11-diethyl-3
Carbonic acid, [4-[[(2S)-2-(4-aminobutyl)-35-[4-[[[[4-[(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)methyl]cyclohexyl]carbonyl]amino]methyl]-1H-1,2,3-triazol-1-yl]-1,4,8-trioxo-6,12,15,18,21,24,27,30,33-nonaoxa-3,9-diazapentatriacont-1-yl]amino]phenyl]methyl (4S)-4,11-diethyl-3,4,12,14-tetrahydro-9-hydroxy...
4-[[(2S)-2-(4-Aminobutyl)-35-[4-[[[[4-[(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)methyl]cyclohexyl]carbonyl]amino]methyl]-1H-1,2,3-triazol-1-yl]-1,4,8-trioxo-6,12,15,18,21,24,27,30,33-nonaoxa-3,9-diazapentatriacont-1-yl]amino]phenyl]methyl(4S)-4,11-diethyl-3,4,12,14-tetrahydro-9-hydroxy-3,14-dioxo-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-4-yl carbonate | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C73H97N11O22 | [MDL Number]
MFCD32701926 | [MOL File]
1279680-68-0.mol | [Molecular Weight]
1480.61 |
| Chemical Properties | Back Directory | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C | [solubility ]
DMSO: 100 mg/mL (67.54 mM) | [form ]
Solid | [pka]
9.12±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
CL2A-SN38 is a SN38 derivative with a Mal-PEG attached peptide linker, it can easily react with antibody to form an antibody-drug conjugate (ADC). SN-38 is a potent DNA Topoisomerase I inhibitor. CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A linker is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. | [Uses]
CL2A-SN-38 is a agent-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody agent conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A-SN-38 uses hydrolyzable linker to deliver active agents within tumor cells and in the tumor microenvironment, resulting in bystander effects[1]. | [in vivo]
CL2A-SN-38 coupled to the anti-Trop-2 humanized antibody hRS7 (intraperitoneal injection, 0.2 or 0.4 mg/kg, twice weekly, 4 weeks) can both significantly inhibit tumor growth in mice with human colon (COLO 205) or pancreatic (Capan-1) tumour xenografts[2].
| [IC 50]
Camptothecins | [storage]
-20°C, stored under nitrogen, away from moisture | [References]
[1] Cardillo TM, et al. Humanized anti-Trop-2 IgG-SN-38 conjugate for effective treatment of diverse epithelial cancers: preclinical studies in human cancer xenograft models and monkeys. Clin Cancer Res. 2011 May 15;17(10):3157-69. DOI:10.1158/1078-0432.CCR-10-2939
[2] Thomas M Cardillo, et al. Humanized anti-Trop-2 IgG-SN-38 conjugate for effective treatment of diverse epithelial cancers: preclinical studies in human cancer xenograft models and monkeys. Clin Cancer Res. 2011 May 15;17(10):3157-69. DOI:10.1158/1078-0432.CCR-10-2939 |
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