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Merck
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SML2672

Sigma-Aldrich

Tandutinib hydrochloride

≥98% (HPLC)

同義詞:

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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About This Item

經驗公式（希爾表示法）:
C31H42N6O4 · xHCl
CAS號碼:
387867-13-2
分子量：:
562.70 (free base basis)
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

儲存條件

desiccated

顏色

white to beige

溶解度

H2O: 2 mg/mL, clear

儲存溫度

2-8°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 密鑰

UXXQOJXBIDBUAC-UHFFFAOYSA-N

生化／生理作用

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.

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

分析證明 (COA)

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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
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
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
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
Louise M Kelly et al.
Cancer cell, 1(5), 421-432 (2002-07-19)
Up to 30% of acute myelogenous leukemia (AML) patients harbor an activating internal tandem duplication (ITD) within the juxtamembrane domain of the FLT3 receptor, suggesting that it may be a target for kinase inhibitor therapy. For this purpose we have
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