产品名称

坦度替尼(Tandutinib (MLN518))

一般描述

Tandutinib(坦度替尼) is a potent FLT3 antagonist.

别 称

4-[6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-yl]-N-(4-propan-2-yloxyphenyl)piperazine-1-carboxamide; CT 53518; NSC726292

纯 度

≥98.0%(HPLC)

CAS NO.

387867-13-2

分子式

C³¹H⁴²N⁶O⁴

分子量

562.7

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体 

溶解性(25℃)

DMSO

~5mg/mL

乙醇

≥5mg/mL

水

Insoluble

l  生物学信息

生物活性/药理作用

MLN518 is a novel quinazoline-based small molecule inhibitor of the FLT3, KIT, and platelet-derived growth-factor receptor (PDGFR) tyrosine kinases with that has been shown to have great efficacy in murine models of FLT3 ITD-positive leukemia. Experiments with mice demonstrate that at effective concentrations, MLN518 has mild toxicity toward normal hematopoiesis for FLT3 ITD-positive leukemia. MLN518 has also been shown to preferentially inhibit the growth of blast colonies from FLT3 ITD-positive as compared to ITD-negative patients with AML, without significantly affecting colony formation by normal human progenitor cells.

Tandutinib (MLN518, CT53518) is a potent  FLT3 antagonist with IC50 of 0.22 μM, also inhibits PDGFR and c-Kit, 15 to 20-fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR and KDR.

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov