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- 產(chǎn)品名稱： Calicheamicin γ1
- 產(chǎn)品貨號(hào)： CS0015
- 貨期： 現(xiàn)貨
- 價(jià)格與訂購： 8650
- 數(shù)量：
庫存： 10
- 規(guī)格： 10mg
- 產(chǎn)品信息
- 如何訂購
產(chǎn)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.
靶點(diǎn)活性
Calicheamicins
體外活性
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].
體內(nèi)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.
別名
Calicheamicin γ1 , 卡奇霉素
分子量
1368.35
分子式
C55H74IN3O21S4
CAS No.
108212-75-5
存儲(chǔ)
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 )
參考文獻(xiàn)
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 .
上一篇 FR901464
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