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MTI-31
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MTI-31图片
CAS NO:1567915-38-1
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
MTI-31 是一种有效的,具有口服活性的,且高度选择性的mTORC1mTORC2抑制剂。MTI-31 高选择性作用于 mTOR,Kd为 0.20 nM。MTI-31 对 mTOR 的IC50为 39 nM。MTI-31可用于乳腺癌的研究。
生物活性

MTI-31 is a potent, orally active and highly selective inhibitor ofmTORC1andmTORC2. MTI-31 is selective formTOR(Kd: 0.20 nM) versus PIK3CA, PIK3CB and PIK3G with >5,000 fold selectivity inmTORbinding assays. MTI-31 shows anIC50of 39 nM formTORin LANCE assay ofmTORsubstrate phosphorylation with 100 μM ATP. MTI-31 can be used for the research of breastcancer[1].

IC50& Target[1]

mTOR

0.2 nM (Ki)

mTOR

39 nM (IC50, 100 μM ATP)

mTORC1

 

mTORC2

 

体外研究
(In Vitro)

MTI-31 acts as a potent and selective inhibitor of mTOR enzymatic activity capable of targeting both mTORC1 and mTORC2 functions in cancer cells[1].
MTI-31 (0.01-100 μM) elicits a potent and more substantial inhibition of cell growth than that of Rapamycin[1].
Treatment with MTI-31 for 6 h demonstrates a dose-dependent inhibition of both the mTORC1 substrates P-S6K1(T389), P-S6(S235/6), P-4EBP1(T70) and mTORC2 substrate P-AKT(S473), achieving 50% inhibition at ≤0.12 μM in three representative tumor cell lines harboring mTOR pathway dysregulation (786-O renal, U87MG glioma and MDA-MB-453 breast)[1].
MTI-31-induced apoptosis requires mTORC2-regulated Bim- and GSK3 activity[1].

Cell Proliferation Assay[1]

Cell Line:MDA-MB-453 cells
Concentration:0.01, 0.1, 1, 10, 100 μM
Incubation Time:3 days
Result:Significantly inhibited cellular proliferation after treatment for 3 days.

Western Blot Analysis[1]

Cell Line:786-O renal, U87MG glioma and MDA-MB-453 breast cells
Concentration:0.12, 0.37, 1.11, 3.33, 10 μM
Incubation Time:6 hours
Result:Demonstrated a dose-dependent inhibition of both the mTORC1 substrates P-S6K1(T389), P-S6(S235/6), P-4EBP1(T70) and mTORC2 substrate P-AKT(S473).
体内研究
(In Vivo)

MTI-31 is a potent mTOR inhibitor in vivo and elicits strong antitumor efficacy. MTI-31(5-40 mg/kg; orally) is efficacious in several tumor models harboring HER2+/PIK3CAmut and/or PTEN-deficiency exemplified by MDA-MB-453 and 786-O[1].
Treatment of tumor bearing nude mice with orally administered MTI-31 inhibits growth of H1975 tumors (25 mg/kg/d; orally) or U87MG tumors (30 mg/kg/d; orally)[2].

Animal Model:Female nude mice bearing tumors of MDA-MB-453, 786-O or HCC1806[1]
Dosage:2.5, 5, 10, 20, 40 mg/kg for MDA-MB-453 and 786-O; 20 and 40 mg/kg for HCC1806
Administration:Treated orally via a once daily (qd) regimen
Result:Was efficacious in several tumor models harboring HER2+/PIK3CAmut and/or PTEN-deficiency exemplified by MDA-MB-453 and 786-O. Demonstrated a dose proportional tumor growth inhibition (TGI) with a minimum efficacious dose (MED) of 5 mg/kg (>50% TGI, p<0.01) and a maximum tolerated dose (MTD) of 40 mg/kg (7-15% body weight loss without mortality).
In contrast, had limited efficacy in the HER2-/PIK3CAwt HCC1806 breast tumor model even at the highest 40 mg/kg.
分子量

474.55

性状

Solid

Formula

C26H30N6O3

CAS 号

1567915-38-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 8.33 mg/mL(17.55 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1073 mL10.5363 mL21.0726 mL
5 mM0.4215 mL2.1073 mL4.2145 mL
10 mM0.2107 mL1.0536 mL2.1073 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 0.83 mg/mL (1.75 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (1.75 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。