计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Taltobulin
有货
为什么选择此级别
Moligand™ 级 提供 ≥98% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存,充氩,干燥。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Taltobulin (HTI-286), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis
In Vitro
Taltobulin (HTI-286; 0.2-7.3 nM; 3 days) inhibits the growth of 18 tumor cell lines (leukemia, ovarian, NSCLC, breast, colon, and melanoma cell lines) with an average IC 50 of 2.5±2.1 nM and a median value of 1.7 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Leukemia CCRF-CEM cell line; ovarian 1A9 cell line; NSCLC A549 and NCI-H1299 cell lines; breast MX-1W and MCF-7 cell lines; colon HCT-116, DLD-1, Colo205, KM20, SW620, S1, HCT-15 and Moser cell lines; melanoma A375, Lox and SK-Mel-2 cell lines Concentration: 0.2-7.3 nM Incubation Time: 3 days Result: Inhibited the growth of tumor cell lines with IC 50 s of 0.2±0.03 nM (for leukemia CCRF-CEM cell line), 0.6±0.1 nM (for ovarian 1A9 cell line), 1.1±0.5 and 6.8±6.1 nM ( for NSCLC A549 and NCI-H1299 cell lines), 1.8±0.6, 7.3±2.3 nM (for breast MX-1W, MCF-7 cell lines), 0.7±0.2, 1.1±0.4, 1.5±0.6, 1.8±0.6, 3.6±0.8, 3.7±2.0, 4.2±2.5, and 5.3±4.1 nM ( for colon HCT-116, DLD-1, Colo205, KM20, SW620, S1, HCT-15, and Moser cell lines), 1.1±0.8, 1.4±0.6 and 1.7±0.5 nM (for melanoma A375, Lox and SK-Mel-2 cell lines).
In Vivo
Taltobulin (HTI-286; 1.6 mg/kg i.v.) inhibits the growth of human tumor xenografts (e.g., HCT-15, DLD-1, MX-1W, and KB-8-5) in athymic nu/nu female mice . ?\nTaltobulin (HTI-286; 3 mg/kg; p.o. gavage) inhibits growth by 97.3 % and 82% in athymic nu/nu female mice with Lox melanoma xenografts and KB-3-1 epidermoid xenograft model, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Athymic nu/nu female mice with Lox melanoma model (5-6 weeks of age) Dosage: 1.6 mg/kg Administration: Administered i.v.;for 35 days Result: Growth of Lox tumors was inhibited by 96-98% on day 12 compared with vehicle-treated controls. Growth of KB-8-5 tumors was inhibited by 84% on day 14 compared with vehicle-treated controls. Growth of MX-1W tumors was inhibited by 97% compared with vehicle-treated controls. Growth of DLD-1 and HCT-15 tumors was inhibited by 80 and 66%, respectively.
Form:Solid
IC50& Target:Traditional Cytotoxic Agents
规格
别名
塔托布林 | HTI-286 | SPA-110 | 他托布林 | (S,E)-2,5-二甲基-4-((S)-N,3,3-三甲基-2-((S)-3-甲基-2-(甲氨基)-3-苯基丁酰胺基)丁酰胺基)己-2-烯酸
英文别名
HTI-286 | SPA-110 | (S,E)-2,5-Dimethyl-4-((S)-N,3,3-trimethyl-2-((S)-3-methyl-2-(methylamino)-3-phenylbutanamido)butanamido)hex-2-enoic acid
规格或纯度
Moligand™, ≥98%
英文名称
Taltobulin
生化机理
Taltobulin（HTI-286）是三肽 hemiasterlin 的合成类似物，是一种强效抗微管药物，可在体外和体内规避 P 糖蛋白介导的抗药性。Taltobulin 可抑制纯化的微管蛋白的聚合，破坏微管蛋白在细胞内的聚合。
储存条件
-20°C储存,充氩,干燥
运输条件
超低温运输
作用类型
抑制剂
纯度
≥98%
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(C)[C@@H](/C=C(\C)/C(=O)O)N(C)C(=O)[C@H](C(C)(C)C)NC(=O)[C@H](C(C)(C)C1=CC=CC=C1)NC
PubChem CID
分子量
473.65
技术文档
高级数据
关联靶点（人）
TUBB1
Tclin
微管蛋白β-1链(Tubulin beta-1 chain)
(1 活性数据)
TUBB1
Tclin
Tubulin beta-1 chain
(182 活性数据)
1A9
(618 活性数据)
KB 3-1
(1143 活性数据)
MCF7
(126967 活性数据)
NCI-H1299
(3248 活性数据)
HepG2
(196354 活性数据)
KB
(17409 活性数据)
LOX IMVI
(44321 活性数据)
HCT-15
(51914 活性数据)
关联靶点（其它种属）
Hdac6
Histone deacetylase 6 (222 活性数据)
beta-tubulin
Beta tubulin (90 活性数据)
| 活性类型 | Relation | Activity value | Units | Action Type | 期刊 | PubMed Id | doi | Assay Aladdin ID |
|---|
Bos taurus (956 活性数据)
Mus musculus (284745 活性数据)
Rattus norvegicus (775804 活性数据)
rep
Replicase polyprotein 1ab (378 活性数据)
SARS-CoV-2 (38078 活性数据)
作用机制
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
化学和物理性质
溶解性
DMSO : ≥ 100 mg/mL (211.13 mM)
分子量
473.600 g/mol
XLogP3
2.600
氢键供体数Hydrogen Bond Donor Count
3
氢键受体数Hydrogen Bond Acceptor Count
5
可旋转键计数Rotatable Bond Count
11
精确质量Exact Mass
473.325 Da
单同位素质量Monoisotopic Mass
473.325 Da
拓扑极表面积Topological Polar Surface Area
98.700 Ų
重原子数Heavy Atom Count
34
形式电荷Formal Charge
0
复杂度Complexity
745.000
同位素原子数Isotope Atom Count
0
定义的原子立体中心计数Defined Atom Stereocenter Count
3
未定义的原子立体中心计数Undefined Atom Stereocenter Count
0
定义的键立体中心计数Defined Bond Stereocenter Count
1
未定义的键立体中心计数Undefined Bond Stereocenter Count
0
所有立体化学键的总数The total count of all stereochemical bonds
1
共价键合单元计数Covalently-Bonded Unit Count
1
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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