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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
Calicheamicin γ1
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
108212-75-5
- 规格：
10 mM * 1 mL/1 mg/5 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥ |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥2800.0 |
| 规格： | 5 mg | 产品价格： | ￥5600.0 |
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Calicheamicin
CAS No. : 108212-75-5
MCE 国际站：Calicheamicin
产品活性：Calicheamicin 是一种肿瘤抗生素，也是有效的细胞毒性试剂，可引起DNA双链断裂。Calicheamicin 抑制 DNA 合成。
研究领域：Cell Cycle/DNA Damage | Antibody-drug Conjugate/ADC Related | Anti-infection | Apoptosis
作用靶点：DNA Alkylator/Crosslinker | ADC Cytotoxin | Bacterial | Apoptosis | Antibiotic
In Vitro: 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). CMC-544, consisting of a humanized CD22 Ab linked to calicheamicin, is effective in pediatric primary B-cell precursor acute lymphoblastic leukemia (BCP-ALL) cells in vitro. CMC-544 induces cell death in various ALL cell lines in a dose- and time-dependent way, with IC50 values ranging from 0.15 to 4.9 ng/mL. CMC-544 (10 ng/mL) is effective and specific in primary BCP-ALL cells. In CMC-544-treated cells, the level of CD22 has decreased relative to that on G5/44-treated cells and continued to decrease.
In Vivo: 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. PF-06647263 (0.27, 0.36 mg/kg) results in significant tumor regressions in TNBC xenografts.
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