卡利奇霉素
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- CAS号:
- 108212-75-5
- 英文名:
- Calicheamicin
- 英文别名:
- CS-2391;calicimycin;Calicheamicin;Calicheamicin γ1;Calicheamicin g1;calicheamicin γ1I;Calicheamicin g1I;Card spectinomycin;Calichemicin gamma1;calicheamicin gamma
- 中文名:
- 卡利奇霉素
- 中文别名:
- 凯立霉素;刺孢霉素;卡奇霉素;卡利奇霉素;卡里奇霉素;卡奇霉素Γ1;加利西霉素Γ1;凯立霉素 Γ1;卡利奇霉素/卡奇霉素;化合物 T14858
- CBNumber:
- CB01353750
- 分子式:
- C55H74IN3O21S4
- 分子量:
- 1368.34
- MOL File:
- 108212-75-5.mol
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卡利奇霉素化学性质
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比旋光度:
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D26 -124° (c = 0.98%, EtOH)
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密度:
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1.57±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO : ≥ 100 mg/mL (73.08 mM);Water : < 0.1 mg/mL (insoluble)
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形态:
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Solid
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酸度系数(pKa):
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7.13±0.60(Predicted)
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颜色:
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White to yellow
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卡利奇霉素性质、用途与生产工艺
卡奇霉素（calicheamicins，CLM）是从稀有放线茵小单孢菌发酵液中分离得到的烯二炔类抗肿瘤抗生素。
卡奇霉素的生物活性浓度＜1 Pg·mL-1，对白血病如淋巴细胞白血病P388和L1210细胞以及实体瘤如结肠癌26和黑色素瘤B-16细胞有极强的杀伤作用。卡奇霉素生物活性的发挥主要通过与细胞DNA特异序列的小沟结合，直接断裂细胞DNA，进一步诱导肿瘤细胞凋亡，同时，卡奇霉素对细胞RNA也有非特异性的损伤作用，卡奇霉素与抗CD33单抗偶联物Mylotarg是第一个被FDA批准用于肿瘤治疗的单抗导向药物，已在临床应用。
卡奇霉素是一种有效的细胞毒性试剂,可引起DNA双链断裂。
卡奇霉素有剧毒，是土壤细菌产生的数百种代谢物之一。
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。
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 (EC
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= 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 IC
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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.
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.
卡利奇霉素
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/11/08 | HY-19609 | 卡利奇霉素
Calicheamicin | | 1 mg | 2800元 |
| 2024/11/08 | HY-19609 | 卡利奇霉素
Calicheamicin | | 10 mM * 1 mLin DMSO | 20772元 |
108212-75-5, 卡利奇霉素 相关搜索:
- Pharmaceutical
- ADC
- 抗体类配体
- 医用原料
- 抑制剂
- 化学试剂
- 其他
- 试剂
- 原料药及中间体
- 原料药
- 科研原药系列
- 医药原料药
- 原料药【仅供科研】
- C55H74IN3O21S4
- S-((2R,3S,4S,6S)-6-((((2R,3S,4S,5R,6R)-5-(((2S,4S,5S)-5-(乙基氨基)-4-甲氧基四氢-2H-吡喃-2-基)氧基)-4-羟基-6-(((2S,5Z,9R,13E)-9-羟基-12-((甲氧羰基)氨基)-13-(2-(甲基三硫烷基)乙亚基)-11-氧代双环[7.3.1]十三碳-1(12),5-二烯-3,7-二炔-2-基)氧基)-2-甲基四氢-2H-吡喃-3-基)氨基)氧基)-4-羟基-2-甲基四氢-2H-吡喃-3-基) 4-(((2S,3R,4
- S-((2R,3S,4S,6S)-6-((((2R,3S,4S,5R,6R)-5-(((2S,4S,5S)-5-(乙基氨基)-4-甲氧基四氢-2H-吡喃-2-基)氧基)-4-羟基-6-(((2S,5Z,9R,13E)-9-羟基-12-((甲氧羰基)氨基)-13-(2-(甲基三硫烷基)乙亚基)-11-氧代双环[7.3.1]十三碳-1(12),5-二烯-3,7-二炔-2-基)氧基)-2-甲基四氢-2H-吡喃-3-基)氨基)氧基)-4-羟基-2-甲基四氢-2H-吡喃-3-基) 4-(((2S,3R,4R,5S,6S)-3,5-二羟基-4-甲氧基-6-甲基四氢-2H-吡喃-2-基)氧基)-3-碘-5,
- 凯立霉素 Γ1
- 卡利奇霉素/卡奇霉素
- 化合物 T14858
- 凯立霉素
- 卡里奇霉素
- 卡奇霉素Γ1
- CALICHEAMICIN卡利奇霉素
- 加利西霉素Γ1
- 刺孢霉素
- 卡奇霉素
- 卡利奇霉素
- 卡奇霉素 GAMMA1
- 108212-75-5
- Calicheamicin
- S-((2R,3S,4S,6S)-6-((((2R,3S,4S,5R,6R)-5-(((2S,4S,5S)-5-(ethylamino)-4-methoxytetrahydro-2H-pyran-2-yl)oxy)-4-hydroxy-6-(((2S,5Z,9R,13E)-9-hydroxy-12-((methoxycarbonyl)amino)-13-(2-(methyltrisulfaneyl)ethylidene)-11-oxobicyclo[7.3.1]trideca-1(12),5-dien-3,7-diyn-2-yl)oxy)-2-methyltetrahydro-2H-pyran-3-yl)amino)oxy)-4-hydroxy-2-methyltetrahydro-2H-pyran-3-yl) 4-(((2S,3R,4R,5S,6S)-3,5-dihydroxy-4-methoxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-3-iodo-5,6-dimethoxy-2-methylbenzothioate
- calicimycin
- Calicheamicin,ADC Cytotoxin,Bacterial,Inhibitor,Apoptosis,inhibit,ADC Payload,Calicheamicin γ 1,DNA Alkylator/Crosslinker,Calicheamicin γ-1,Antibiotic
- Calicheamicin/Calicheamicin γ1
- Card spectinomycin
- Calicheamicin g1
- Carbamic acid,N-[(1R,4Z,8S,13E)-8-[[4,6-dideoxy-4-[[[2,6-dideoxy-4-S-[4-[(6-deoxy-3-O-methyl-a-L-mannopyranosyl)oxy]-3-iodo-5,6-dimethoxy-2-methylbenzoyl]-4-thio-b-D-ribo-hexopyranosyl]oxy]amino]-2-O-[2,4-dideoxy-4-(ethylamino)-3-O-methyl-a-L-threo-pentopyranosyl]-b-D-glucopyranosyl]oxy]-1-hydroxy-13-[2-(methyltrithio)ethylidene]-11-oxobicyclo[7.3.1]trideca-4,9-diene-2,6-diyn-10-yl]-,methyl ester
- calicheamicin gamma(1)I USP/EP/BP
- Carbamic acid,N-[(1R,4Z,8S,13E)-8-[[4,6-dideoxy-4-[[[2,6-dideoxy-4-S-[4-[(6-deoxy-3-O-methyl-a-L-mannopyranosyl)oxy]-3-iodo-5,6-dimethoxy-2-methylbenzoyl]-4-thio-b-D-ribo-hexopyranosyl]oxy]amino]-2-O-[2,4-dideoxy-4-(ethylamino)-3-O-methyl-a-L-threo-pentop
- Carbamic acid, N-[(1R,4Z,8S,13E)-8-[[4,6-dideoxy-4-[[[2,6-dideoxy-4-S-[4-[(6-deoxy-3-O-methyl-α-L-mannopyranosyl)oxy]-3-iodo-5,6-dimethoxy-2-methylbenzoyl]-4-thio-β-D-ribo-hexopyranosyl]oxy]amino]-2-O-[2,4-dideoxy-4-(ethylamino)-3-O-methyl-α-L-threo-pentopyranosyl]-β-D-glucopyranosyl]oxy]-1-hydroxy-...
- CS-2391
- calicheamicin γ1I
- Calicheamicin gamma1
- Calicheamicin g1I
- Calicheamicin γ1 purity>95
- calicheamicin gamma
- LL-E 33288 gamma1-I
- Calicheamicin γ1
- Carbamic acid, ((1R,4Z,8S,13E)-8-((4,6-dideoxy-4-(((2,6-dideoxy-4-S-(4-((6-deoxy-3-o-methyl-alpha-L-mannopyranopyranosyl)oxy)-3-iodo-5,6-dimethoxy-2-methylbenzoyl)-4-thio-beta-D-ribo-hexopyranosyl)oxy)amino)-2-o-(2,4-dideoxy-4-(ethylamino)-3-o-methyl-alpha-L-threo-pentopyranosyl)-beta-D-glucopyranosyl)oxy)-1-hydroxy-13-(2-(methyltrithio)ethylidene)-11-oxobicyclo(7.3.1)trideca-4,9-diene-2,6-diyn-10-yl)-, methyl ester
- Calichemicin gamma1
- Benzenecarbothioic acid, 4-((6-deoxy-3-o-methyl-alpha-L-mannopyranosyl)oxy)-3-iodo-5,6-dimethoxy-2-methyl-, 4''-ester with methyl (8-((4,6-dideoxy-2-o-(2,4-dideoxy-4-(ethylamino)-3-o-methyl-alpha-L-threo-pentapyranosyl)-4-(((2,6-dideoxy-4-thio-beta-D-ribo-hexopyranosyl)oxy)amino)-beta-D-glucopyranosyl)oxy)-1-hydroxy-13-(2-(methyltrithio)ethylidene)-11-oxobicyclo(7.3.1)trideca-4,9-diene-2,6-diyn-10-yl)carbamate, (1R-(1R*,4Z,8S*,13E))-
- calicheamicin gamma(1)I