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Merck
CN

SML2672

Sigma-Aldrich

Tandutinib hydrochloride

≥98% (HPLC)

别名:

4-[6-Methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinyl]-N-[4-(1-methylethoxy)phenyl]-1-piperazinecarboxamide hydrochloride, CT 53518 hydrochloride, CT-53518 hydrochloride, CT53518 hydrochloride, MLN 518 hydrochloride, MLN-518 hydrochloride, MLN518 hydrochloride, N-(4-Isopropoxyphenyl)-4-(6-methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-yl)piperazine-1-carboxamide hydrochloride

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关于此项目

经验公式（希尔记法）:
C31H42N6O4 · xHCl
化学文摘社编号:
387867-13-2
分子量:
562.70 (free base basis)
UNSPSC代码:
12352200
NACRES:
NA.77

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方案

≥98% (HPLC)

表单

powder

储存条件

desiccated

颜色

white to beige

溶解性

H2O: 2 mg/mL, clear

储存温度

2-8°C

SMILES字符串

N5(CCCCC5)CCCOc1cc2ncnc(c2cc1OC)N3CCN(CC3)C(=O)Nc4ccc(cc4)OC(C)C

InChI

1S/C31H42N6O4/c1-23(2)41-25-10-8-24(9-11-25)34-31(38)37-17-15-36(16-18-37)30-26-20-28(39-3)29(21-27(26)32-22-33-30)40-19-7-14-35-12-5-4-6-13-35/h8-11,20-23H,4-7,12-19H2,1-3H3,(H,34,38)

InChI key

UXXQOJXBIDBUAC-UHFFFAOYSA-N

相关类别

生化/生理作用

Orally active, potent βPDGFR, c-Kit, Flt3 (Flk2, Stk1) receptor tyrosine kinase inhibitor with anti-leukemia efficacy in vitro and in vivo.
Tandutinib (CT53518, MLN518) is a potent receptor tyrosine kinase inhibitor against PDGFRβ, c-Kit, Flt3 (IC50 = 0.20, 0.17, 0.22, 3.43 μM, respectively, against 8 nM PDGF-BB induced autophosphorylation of βPDGFR, βPDGFR/c-Kit, βPDGFR/Flt3, βPDGFR/CSF-1R chimera expressed in CHO cells; IC50 =30 μM against KDR, EFGR, FGFR, InsR, Abl, Src, PKA, PKC, ERK2, MEK1, MKK4/6, p38). Tandutinib prolongs the survival in murine CMML (Baf3 with Tel/βPDGFR chimera) and Flt-3/ITD AML leukemia models (60 mg/kg bid p.o.) with good oral bioavailability.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000076353
0000076354
0000072557

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Nimitha R Mathew et al.
Nature medicine, 24(3), 282-291 (2018-02-13)
Individuals with acute myeloid leukemia (AML) harboring an internal tandem duplication (ITD) in the gene encoding Fms-related tyrosine kinase 3 (FLT3) who relapse after allogeneic hematopoietic cell transplantation (allo-HCT) have a 1-year survival rate below 20%. We observed that sorafenib
Sivapriya Ponnurangam et al.
Molecular cancer therapeutics, 12(5), 598-609 (2013-02-22)
The c-Kit receptor can activate distinct signaling pathways including phosphoinositide 3-kinase (PI3K)/Akt and mTOR. Aberrant c-Kit activation protects cells from apoptosis and enhances invasion of colon carcinoma cells. Tandutinib is a novel quinazoline-based inhibitor of the type III receptor tyrosine
Xiao-qin Zhao et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 49(3), 441-450 (2013-04-27)
Tandutinib is a novel inhibitor of tyrosine kinases FLT3, PDGFR and KIT. Our study was to explore the capability of tandutinib to reverse ABC transporter-mediated multidrug resistance. Tandutinib reversed ABCG2-mediated drug resistance in ABCG2-482-R2, ABCG2-482-G2, ABCG2-482-T7 and S1-M1-80 cells and
Wen Deng et al.
Oncology reports, 29(6), 2479-2485 (2013-03-26)
It is well established that ATP-binding cassette (ABC) transporter-mediated multidrug resistance (MDR) is one of the major mechanisms that causes resistance to antineoplastic drugs in cancer cells. ABC transporters can significantly decrease the intracellular concentration of antineoplastic drugs by increasing
Ian J Griswold et al.
Blood, 104(9), 2912-2918 (2004-07-10)
Internal tandem duplications (ITDs) of the FMS-like tyrosine kinase 3 (FLT3) receptor tyrosine kinase are found in approximately 30% of patients with acute myelogenous leukemia (AML) and are associated with a poor prognosis. FLT3 ITD mutations result in constitutive kinase
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