卡利奇霉素
| 中文名稱 | 卡利奇霉素 |
|---|---|
| 中文同義詞 | 卡奇霉素 GAMMA1;卡利奇霉素;卡奇霉素;刺孢霉素;加利西霉素Γ1;CALICHEAMICIN卡利奇霉素;卡奇霉素Γ1;卡里奇霉素 |
| 英文名稱 | Calicheamicin |
| 英文同義詞 | calicheamicin gamma(1)I;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))-;Calichemicin gamma1;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;Calicheamicin γ1;LL-E 33288 gamma1-I;calicheamicin gamma;Calicheamicin γ1 purity>95 |
| CAS號(hào) | 108212-75-5 |
| 分子式 | C55H74IN3O21S4 |
| 分子量 | 1368.34 |
| EINECS號(hào) | |
| 相關(guān)類別 | 原料藥【僅供科研】;醫(yī)藥原料藥;科研原藥系列;原料藥;原料藥及中間體;試劑;其他;化學(xué)試劑;ADC;Pharmaceutical |
| Mol文件 | 108212-75-5.mol |
| 結(jié)構(gòu)式 |  |
卡利奇霉素 性質(zhì)
| 比旋光度 | D26 -124° (c = 0.98%, EtOH) |
|---|---|
| 密度 | 1.57±0.1 g/cm3(Predicted) |
| 儲(chǔ)存條件 | Store at -20°C |
| 溶解度 | DMSO：≥ 100 mg/mL (73.08 mM)；水：< 0.1 mg/mL（不溶） |
| 形態(tài) | 固體 |
| 酸度系數(shù)(pKa) | 7.13±0.60(Predicted) |
| 顏色 | 白色至黃色 |
| InChIKey | HXCHCVDVKSCDHU-PENQSKQENA-N |
卡奇霉素（calicheamicins，CLM）是從稀有放線茵小單孢菌發(fā)酵液中分離得到的烯二炔類抗腫瘤抗生素。
卡奇霉素的生物活性濃度＜1 Pg·mL-1，對(duì)白血病如淋巴細(xì)胞白血病P388和L1210細(xì)胞以及實(shí)體瘤如結(jié)腸癌26和黑色素瘤B-16細(xì)胞有極強(qiáng)的殺傷作用?？ㄆ婷顾厣锘钚缘陌l(fā)揮主要通過與細(xì)胞DNA特異序列的小溝結(jié)合，直接斷裂細(xì)胞DNA，進(jìn)一步誘導(dǎo)腫瘤細(xì)胞凋亡，同時(shí)，卡奇霉素對(duì)細(xì)胞RNA也有非特異性的損傷作用，卡奇霉素與抗CD33單抗偶聯(lián)物Mylotarg是第一個(gè)被FDA批準(zhǔn)用于腫瘤治療的單抗導(dǎo)向藥物，已在臨床應(yīng)用。卡奇霉素是一種有效的細(xì)胞毒性試劑,可引起DNA雙鏈斷裂。
卡奇霉素有劇毒，是土壤細(xì)菌產(chǎn)生的數(shù)百種代謝物之一。
Calicheamicin 是一種腫瘤抗生素，也是有效的細(xì)胞毒性試劑，可引起DNA雙鏈斷裂。Calicheamicin 抑制 DNA 合成。|
Calicheamicins
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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 50 = 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 50 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.
安全信息
| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
|---|---|---|---|---|---|
| 2026/06/05 | HY-19609 | 卡利奇霉素 Calicheamicin | 108212-75-5 | 1 mg | 2800元 |
| 2026/06/05 | HY-19609 | 卡利奇霉素 Calicheamicin | 108212-75-5 | 5 mg | 5600元 |