Tandutinib (MLN518) HCl
目录号 : GC12251
FLT3 inhibitor,potent and selective
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tandutinib, also known as MLN518 or CT53518, is a potent antagonist for FLT3, platelet-derived growth factor receptor (PDGFR), and c-Kit [1].
FLT3 is expressed on the surface of many hematopoietic progenitor cells. Signalling of FLT3 is important for the normal development of haematopoietic stem cells and progenitor cells. High levels of wild-type FLT3 have been observed in some AML patients and may be associated with worse prognosis.
Tandutinib potently inhibited the activity of FLT3, PDGFR, and c-Kit with the IC50 value of ~200 nM. Tandutinib showed no significant effects on other tyrosine or serine/threonine kinases. In Ba/F3 cells expressing different FLT3-ITD mutants, Tandutinib inhibited IL-3-independent cell growth and FLT3-ITD autophosphorylation with an IC50 of 10–100 nM. In human FLT3-ITD-positive AML cell lines, Tandutinib induced apoptosis and inhibited FLT3-ITD phosphorylation, cellular proliferation, and signaling through the MAP kinase and PI3 kinase pathways [1]. Tandutinib inhibited phosphorylation of c-Kit, Akt, mTOR, and p70S6 kinase. Tandutinib significantly inhibited the proliferation and colony formation ability of colon cancer cell lines [2]. Tandutinib decreased the expression level of COX-2, VEGF, and interleukin-8. Intraperitoneal administration of tandutinib significantly suppressed growth of colon cancer tumor xenografts. Tandutinib inhibited the expression of cancer-promoting genes COX-2 and VEGF and suppressed the activation of Akt/mTOR signaling proteins in the xenograft tissues [2].
References:
[1] Kelly L M, Yu J C, Boulton C L, et al. CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML)[J]. Cancer cell, 2002, 1(5): 421-432.
[2] Ponnurangam S, Standing D, Rangarajan P, et al. Tandutinib inhibits the Akt/mTOR signaling pathway to inhibit colon cancer growth[J]. Molecular cancer therapeutics, 2013, 12(5): 598-609.
| Cas No. | N/A | SDF | |
| 化学名 | N-(4-isopropoxyphenyl)-4-(6-methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-yl)piperazine-1-carboxamide hydrochloride | ||
| Canonical SMILES | O=C(NC(C=C1)=CC=C1OC(C)C)N2CCN(C(C3=C4)=NC=NC3=CC(OCCCN5CCCCC5)=C4OC)CC2.Cl | ||
| 分子式 | C31H43ClN6O4 | 分子量 | 599.16 |
| 溶解度 | ≥ 59.9mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.669 mL | 8.345 mL | 16.69 mL |
| 5 mM | 0.3338 mL | 1.669 mL | 3.338 mL |
| 10 mM | 0.1669 mL | 0.8345 mL | 1.669 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。