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I1406

Sigma-Aldrich

伊立替康 盐酸盐

powder, ≥97% (HPLC)

别名:

(S)-4,11-二乙基-3,4,12,14-四氢-4-羟基-3,14-二氧代-1H-吡喃并[3′,4′:6,7]中氮茚并[1,2-b]喹啉-9-基酯, CPT-11, [1,4′-联吡啶]-1′-羧酸

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10 G
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About This Item

经验公式（希尔记法）:
C33H38N4O6 · HCl
CAS号:
100286-90-6
分子量:
623.14
MDL编号:
MFCD01862255
UNSPSC代码:
12352204
PubChem化学物质编号:
329815350
NACRES:
NA.77

¥509.32

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产品名称

伊立替康 盐酸盐, topoisomerase inhibitor

生物来源

plant (Fructus camptothecae)

方案

≥97% (HPLC)

表单

powder

溶解性

DMSO: 50 mg/mL

储存温度

2-8°C

SMILES字符串

Cl.CCc1c2CN3C(=O)C4=C(C=C3c2nc5ccc(OC(=O)N6CCC(CC6)N7CCCCC7)cc15)[C@@](O)(CC)C(=O)OC4

InChI

1S/C33H38N4O6.ClH/c1-3-22-23-16-21(43-32(40)36-14-10-20(11-15-36)35-12-6-5-7-13-35)8-9-27(23)34-29-24(22)18-37-28(29)17-26-25(30(37)38)19-42-31(39)33(26,41)4-2;/h8-9,16-17,20,41H,3-7,10-15,18-19H2,1-2H3;1H/t33-;/m0./s1

InChI key

GURKHSYORGJETM-WAQYZQTGSA-N

基因信息

human ... TOP1(7150)

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此商品
473124751347911
Fmoc-Thr(tBu)-OH ≥98.0% (HPLC)

47622

Fmoc-Thr(tBu)-OH

Fmoc-D-Thr(tBu)-OH ≥98.0% (TLC)

47312

Fmoc-D-Thr(tBu)-OH

Fmoc-Thr(Bzl)-OH ≥98.0% (TLC)

47513

Fmoc-Thr(Bzl)-OH

Fmoc-β-Homothr(tBu)-OH ≥96.0% (HPLC)

47911

Fmoc-β-Homothr(tBu)-OH

assay

≥98.0% (HPLC)

assay

≥98.0% (TLC)

assay

≥98.0% (TLC)

assay

≥96.0% (HPLC)

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

optical activity

[α]20/D +16±1°, c = 1% in ethyl acetate

optical activity

[α]20/D −15±1.5°, c = 1% in ethyl acetate

optical activity

-

optical activity

-

Quality Level

100

Quality Level

100

Quality Level

-

Quality Level

-

reaction suitability

reaction type: C-H Activation

reaction suitability

reaction type: Fmoc solid-phase peptide synthesis

reaction suitability

reaction type: Fmoc solid-phase peptide synthesis

reaction suitability

reaction type: Fmoc solid-phase peptide synthesis

应用

盐酸伊立替康用于：:
  • 与5-氟尿嘧啶联合使用，在MDA-MB-231乳腺癌细胞中筛选生长抑制功能。[1]
  • 在高级别阑尾癌（HGA）和低级别阑尾癌（LGA）中筛选化学敏感性。[2]
  • 作为化学治疗剂，与热休克蛋白抑制剂（HPSC1）联合使用，研究对HT29结肠癌细胞的细胞毒性。[3]

生化/生理作用

抗癌药伊立替康是一种前药，在组织羧酸酯酶作用下转化为7-乙基-10-羟基喜树碱（SN-38）——一种有效的DNA拓扑异构酶I抑制剂。通过UDP葡萄糖醛酸转移酶1A1（UGT1A1）的葡萄糖醛酸化作用，可终止该药的作用。
抗癌药伊立替康是一种前药，在组织羧酸酯酶作用下转化为7-乙基-10-羟基喜树碱（SN-38）——一种有效的DNA拓扑异构酶I抑制剂。通过UDP葡萄糖醛酸转移酶1A1（UGT1A1）的葡萄糖醛酸化作用，可终止该药的作用。该药物能增强组织对辐射损伤的敏感性，因此可用于肿瘤的放射治疗。
抗癌药伊立替康是一种前药，在组织羧酸酯酶作用下转化为7-乙基-10-羟基喜树碱（SN-38）——一种有效的DNA拓扑异构酶I抑制剂。通过UDP葡萄糖醛酸转移酶的葡萄糖醛酸化作用，可终止该药的作用。

象形图

Exclamation mark
GHS07

警示用语：

Warning

危险声明

H302

危险分类

Acute Tox. 4 Oral

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

dust mask type N95 (US), Eyeshields, Gloves

    • 历史批次信息供参考:

    分析证书(COA)

    Lot/Batch Number
    WXBF5520V
    WXBF1756V
    WXBD7510V
    WXBD4657V
    WXBD5905V

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    Francesco Crea et al.
    Molecular cancer therapeutics, 8(7), 1964-1973 (2009-06-18)
    Irinotecan is a topoisomerase-I (Top-I) inhibitor used for the treatment of colorectal cancer. DNA demethylating agents, including 5-azacytidine (5-aza), display synergistic antitumor activity with several chemotherapy drugs. 5-Aza may enhance irinotecan cytotoxicity by at least one of the following mechanisms:
    Re-examining HSPC1 inhibitors
    Lee S, et al.
    Cell Stress & Chaperones, 22(2), 293-306 (2017)
    Appendiceal Cancer Patient-Specific Tumor Organoid Model for Predicting Chemotherapy Efficacy Prior to Initiation of Treatment: A Feasibility Study
    Votanopoulos K, et al.
    Annals of Surgical Oncology, 26(1), 139-147 (2019)
    T C Chang et al.
    Cancer chemotherapy and pharmacology, 75(3), 579-586 (2015-01-13)
    To define the dose-limiting toxicity (DLT), maximum tolerated dose (MTD) and pharmacokinetics (PK) of PEP02, a novel liposome-encapsulated irinotecan, in patients with advanced refractory solid tumors. Patients were enrolled in cohorts of one to three to receive escalating dose of
    Olivia Jones et al.
    Scientific reports, 11(1), 8967-8967 (2021-04-28)
    Cholangiocarcinoma (CCA) is a rare biliary tract cancer with a low five-year survival rate and high recurrence rate after surgical resection. Currently treatment approaches include systemic chemotherapeutics such as FOLFIRINOX, a chemotherapy regimen is a possible treatment for severe CCA
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