产品描述

Calicheamicin is an antitumor antibiotic and is a DNA synthesis inhibitor. It also is a cytotoxic agent that causes double-strand DNA breaks.

靶点活性

Calicheamicins

体外活性

PF-06647263 (anti-EFNA4-ADC) is generated via conjugation of hE22 lysine residues to the AcButDMH-N-Ac-calicheamicin-γ1 linker-payload with an average drug-to-antibody ratio (DAR) of 4.6. PF-06647263 elicits antigen- and concentration-dependent cytotoxicity, as exposure to PF-06647263 for 96 hours results in cell death (EC50= appr 1 ng/mL)[1].

体内活性

PF-06647263 (0.27, 0.36 mg/kg) results in significant tumor regressions in TNBC xenografts[1]. An ADC comprising a humanized anti-EFNA4 monoclonal antibody conjugated to the DNA-damaging agent calicheamicin achieves sustained tumor regressions in both TNBC and ovarian cancer PDX in vivo.

别名

Calicheamicin γ1 , 卡奇霉素

分子量

1368.35

分子式

C55H74IN3O21S4

CAS No.

108212-75-5

存储

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

溶解度

DMSO: 100 mg/mL (73.08 mM)

DMSO: 25 mg/mL (18.27 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

参考文献

1. Damelin M, et al. Anti-EFNA4 Calicheamicin Conjugates Effectively Target Triple-Negative Breast and Ovarian Tumor-Initiating Cells to Result in Sustained Tumor Regressions. Clin Cancer Res. 2015 Sep 15;21(18):4165-73

2. de Vries JF, et al. The novel calicheamicin-conjugated CD22 antibody inotuzumab ozogamicin (CMC-544) effectively kills primary pediatric acute lymphoblastic leukemia cells. Leukemia. 2012 Feb;26(2):255-64

3. Takeshita A, et al. CMC-544 (inotuzumab ozogamicin), an anti-CD22 immuno-conjugate of calicheamicin, alters the levels of target molecules of malignant B-cells. Leukemia. 2009 Jul;23(7):1329-36.

Note

For research use only .