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  1. Protein Tyrosine Kinase/RTK Apoptosis
  2. FLT3 c-Kit PDGFR Apoptosis
  3. Tandutinib

Tandutinib  (Synonyms: 坦度替尼; MLN518; CT53518)

目錄號(hào): HY-10202 純度: 99.48%
COA 產(chǎn)品使用指南 技術(shù)支持

Tandutinib (MLN518) 是一種有效和選擇性的 FLT3 的抑制劑,其 IC50 為 0.22 μM,并且還抑制 c-KitPDGFR,其 IC50 分別為 0.17 μM 和 0.20 μM。Tandutinib 可用于急性骨髓性白血病,并具有穿越血腦屏障的能力。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Tandutinib Chemical Structure

Tandutinib Chemical Structure

CAS No. : 387867-13-2

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Customer Review

Other Forms of Tandutinib:

查看 PDGFR 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Tandutinib (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib can be used for acute myelogenous leukemia (AML)[1][2]. Tandutinib has the ability to cross the blood-brain barrier[3].

IC50 & Target[1]

PDGFR

0.2 μM (IC50)

FLT3

0.22 μM (IC50)

c-Kit

0.17 μM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 IC50
> 10000 nM
Compound: MLN-518
Toxicity against human A375 cells after 72 hrs by cell titer-blue assay
Toxicity against human A375 cells after 72 hrs by cell titer-blue assay
[PMID: 19654408]
A549 IC50
14.75 μM
Compound: Tandutinib
Antiproliferative activity against human A549 cells after 72 hrs by MTS assay
Antiproliferative activity against human A549 cells after 72 hrs by MTS assay
[PMID: 27575478]
BaF3 IC50
10 nM
Compound: Tandutinib
Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay
Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay
[PMID: 32659083]
HCT-116 IC50
18.13 μM
Compound: Tandutinib
Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay
Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay
[PMID: 27575478]
HL-60 GI50
> 10 μM
Compound: MLN518
Growth inhibition of human HL60 cells after 48 hrs by XTT assay
Growth inhibition of human HL60 cells after 48 hrs by XTT assay
[PMID: 25108079]
K562 GI50
> 10 μM
Compound: MLN518
Growth inhibition of human K562 cells after 48 hrs by XTT assay
Growth inhibition of human K562 cells after 48 hrs by XTT assay
[PMID: 25108079]
K562 IC50
> 10000 nM
Compound: MLN-518
Antiproliferative activity against FLT3-deficient human K562 cells after 72 hrs by MTT assay
Antiproliferative activity against FLT3-deficient human K562 cells after 72 hrs by MTT assay
[PMID: 27266526]
K562 IC50
9.21 μM
Compound: MLN518
Antiproliferative activity against human K562 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human K562 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 31614258]
Kasumi 1 IC50
0.022 μM
Compound: MLN-518
Antiproliferative activity against human Kasumi-1 cells after 72 hrs by MTT assay
Antiproliferative activity against human Kasumi-1 cells after 72 hrs by MTT assay
[PMID: 20570526]
Leukemia cell IC50
0.29 μM
Compound: 2
Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-ITD mutation assessed as cell viability after 72 hrs by luciferase assay
Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-ITD mutation assessed as cell viability after 72 hrs by luciferase assay
[PMID: 22221201]
Leukemia cell IC50
0.64 μM
Compound: 2
Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing wild type FLT3 assessed as cell viability after 72 hrs by luciferase assay
Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing wild type FLT3 assessed as cell viability after 72 hrs by luciferase assay
[PMID: 22221201]
Leukemia cell IC50
3.4 μM
Compound: 2
Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-D835Y mutation assessed as cell viability after 72 hrs by luciferase assay
Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-D835Y mutation assessed as cell viability after 72 hrs by luciferase assay
[PMID: 22221201]
MCF7 IC50
14.7 μM
Compound: Tandutinib
Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay
[PMID: 27575478]
MOLM-13 GI50
0.052 μM
Compound: MLN518
Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 32975953]
MOLM-13 IC50
0.081 μM
Compound: MLN-518
Antiproliferative activity against human MOLM13 cells after 72 hrs by MTT assay
Antiproliferative activity against human MOLM13 cells after 72 hrs by MTT assay
[PMID: 20570526]
MOLM-13 GI50
1.9 μM
Compound: MLN518
Antiproliferative activity against human MOLM-13 cells harboring D835Y mutant assessed as reduction in cell viability after 72 hrs by MTS assay
Antiproliferative activity against human MOLM-13 cells harboring D835Y mutant assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 32975953]
MOLM-13 IC50
10 nM
Compound: Tandutinib
Antiproliferative activity against human MOLM-13 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay
Antiproliferative activity against human MOLM-13 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay
[PMID: 32659083]
MOLM-14 IC50
10 nM
Compound: Tandutinib
Antiproliferative activity against human MOLM-14 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay
Antiproliferative activity against human MOLM-14 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay
[PMID: 32659083]
MV4-11 IC50
0.055 μM
Compound: MLN518
Cytotoxicity against FLT3-dependent human MV4-11 cells after 72 hrs by MTT assay
Cytotoxicity against FLT3-dependent human MV4-11 cells after 72 hrs by MTT assay
[PMID: 22452518]
MV4-11 IC50
0.06 μM
Compound: MLN518
Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 31614258]
MV4-11 IC50
0.119 μM
Compound: MLN-518
Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay
[PMID: 20570526]
MV4-11 IC50
302 nM
Compound: MLN-518
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant after 72 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant after 72 hrs by MTT assay
[PMID: 27266526]
MV4-11 IC50
60 nM
Compound: MLN-518
Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay
Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay
[PMID: 19654408]
MV4-11 GI50
8.756 μM
Compound: MLN518
Growth inhibition of human MV411 cells after 48 hrs by XTT assay
Growth inhibition of human MV411 cells after 48 hrs by XTT assay
[PMID: 25108079]
P815 IC50
600 nM
Compound: 3
Cytotoxicity in mouse P815 cells expressing KIT D814Y mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity in mouse P815 cells expressing KIT D814Y mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 29678462]
RS4-11 IC50
> 5 μM
Compound: MLN-518
Antiproliferative activity against human RS4:11 cells after 72 hrs by MTT assay
Antiproliferative activity against human RS4:11 cells after 72 hrs by MTT assay
[PMID: 20570526]
RS4-11 IC50
170 nM
Compound: MLN-518
Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
[PMID: 19654408]
RS4-11 IC50
33 nM
Compound: MLN-518
Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
[PMID: 19654408]
Sf9 IC50
0.22 μM
Compound: 19; MLN518, CT53518
Inhibition of N-terminal GST-tagged human FLT3 (563 to 993 residues) cytoplasmic domain expressed in baculovirus infected sf9 cells using EAIYAAPFAKKK as substrate after 10 mins in presence of [gamma-33P]-ATP by scintillation counting method
Inhibition of N-terminal GST-tagged human FLT3 (563 to 993 residues) cytoplasmic domain expressed in baculovirus infected sf9 cells using EAIYAAPFAKKK as substrate after 10 mins in presence of [gamma-33P]-ATP by scintillation counting method
[PMID: 31207462]
THP-1 GI50
> 10 μM
Compound: MLN518
Growth inhibition of human THP1 cells after 48 hrs by XTT assay
Growth inhibition of human THP1 cells after 48 hrs by XTT assay
[PMID: 25108079]
THP-1 IC50
1 μM
Compound: MLN-518
Antiproliferative activity against human THP1 cells after 72 hrs by MTT assay
Antiproliferative activity against human THP1 cells after 72 hrs by MTT assay
[PMID: 20570526]
U-937 IC50
> 5 μM
Compound: MLN-518
Antiproliferative activity against human U937 cells after 72 hrs by MTT assay
Antiproliferative activity against human U937 cells after 72 hrs by MTT assay
[PMID: 20570526]
U-937 IC50
19.8 μM
Compound: MLN518
Antiproliferative activity against human U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 31614258]
WI-38 IC50
> 10000 nM
Compound: MLN-518
Antiproliferative activity against human WI38 cells after 72 hrs by SRB assay
Antiproliferative activity against human WI38 cells after 72 hrs by SRB assay
[PMID: 27266526]
體外研究
(In Vitro)

Tandutinib (0-3 μM; 30 minutes; Ba/F3 cells) treatment inhibits IL-3-independent cell growth and FLT3-ITD autophosphorylation with an IC50 of 10-100 nM in Ba/F3 cells expressing different FLT3-ITD mutants[1].
Tandutinib (1 μM; 24-96 hours; Molm-14 and THP-1 AML cells) treatment induces apoptosis in FLT3-ITD-positive AML cells[1].
In human FLT3-ITD-positive AML cell lines, Tandutinib inhibits FLT3-ITD phosphorylation (IC50 of ~30 nM). As with Erk2, a constitutively high level of Akt phosphorylation is readily detected and is efficiently blocked by pretreatment of the Molm-14 cells with 100-300 nM Tandutinib[1].
Tandutinib inhibits cell proliferation of the FLT3-ITD-positive Molm-13 and Molm-14 with an IC50 of 10 nM. And signaling through the MAP kinase and PI3 kinase pathways[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: Molm-14 and THP-1 AML cells
Concentration: 1 μM
Incubation Time: 24 hours, 48 hours, 72 hours, 96 hours
Result: Induced apoptosis in FLT3-ITD-positive AML cells.

Western Blot Analysis[1]

Cell Line: Ba/F3 cells
Concentration: 0 μM, 0.003 μM, 0.01 μM, 0.03 μM, 0.1 μM, 1 μM and 3 μM
Incubation Time: 30 minutes
Result: In Ba/F3 cells expressing different FLT3-ITD mutants, inhibited IL-3-independent cell growth and FLT3-ITD autophosphorylation.
體內(nèi)研究
(In Vivo)

Tandutinib (60 mg/kg; oral gavage; daily; for 35 days; athymic nude mice) treatment causes a statistically significant increase in survival that was extended on average by 20 days[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Athymic nude mice injected with Ba/F3 cells[1]
Dosage: 60 mg/kg
Administration: Oral gavage; daily; for 35 days
Result: Caused a statistically significant increase in survival that was extended on average by 20 days.
Clinical Trial
分子量

562.70

Formula

C31H42N6O4

CAS 號(hào)
性狀

固體

顏色

White to light yellow

中文名稱

坦度替尼

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 50 mg/mL (88.86 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.7771 mL 8.8857 mL 17.7715 mL
5 mM 0.3554 mL 1.7771 mL 3.5543 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.44 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.44 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購(gòu)。 ,Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL  μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.48%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7771 mL 8.8857 mL 17.7715 mL 44.4286 mL
5 mM 0.3554 mL 1.7771 mL 3.5543 mL 8.8857 mL
10 mM 0.1777 mL 0.8886 mL 1.7771 mL 4.4429 mL
15 mM 0.1185 mL 0.5924 mL 1.1848 mL 2.9619 mL
20 mM 0.0889 mL 0.4443 mL 0.8886 mL 2.2214 mL
25 mM 0.0711 mL 0.3554 mL 0.7109 mL 1.7771 mL
30 mM 0.0592 mL 0.2962 mL 0.5924 mL 1.4810 mL
40 mM 0.0444 mL 0.2221 mL 0.4443 mL 1.1107 mL
50 mM 0.0355 mL 0.1777 mL 0.3554 mL 0.8886 mL
60 mM 0.0296 mL 0.1481 mL 0.2962 mL 0.7405 mL
80 mM 0.0222 mL 0.1111 mL 0.2221 mL 0.5554 mL
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產(chǎn)品名稱:
Tandutinib
目錄號(hào):
HY-10202
需求量: