SMI-4a - CAS:438190-29-5

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SMI-4a (Synonyms:TCS-PIM-1-4a)

目录号 : KCM13808 CAS No. : 438190-29-5 纯度 : ≥98%

Data Sheet SDS 产品使用指南

The serine/threonine Pim kinases have been suggested to promote the activity of the rapamycin-sensitive mammalian target of rapamycin (mTORC1), which regulates cell growth and survival. Pim kinases are overexpressed in solid cancers and hematologic malignancies, and as such have become targets of small molecule inhibitors to prevent the progression of various cancers. SIM-4a is a Pim kinase inhibitor that blocks mTORC1 activity via activation of AMPK. SIM-4a kills a wide range of both myeloid and lymphoid cell lines (with IC values ranging from 0.8 to 40 μM). Incubation of precursor T-cell lymphoblastic leukemia/lymphoma cells with 10 μM SMI-4a induces G phase cell-cycle arrest, dose-dependent induction of p27Kip1, apoptosis through the mitochondrial pathway, and inhibition of the mTORC1 pathway. In immunodeficient mice carrying subcutaneous pre–T-LBL tumors, treatment twice daily with 60 mg/kg SMI-4a causes a significant delay in the tumor growth.

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
5mg		In-stock
10mg		In-stock
50mg		In-stock

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生物活性

SMI-4a is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 μM. SMI-4a also inhibits Pim-2 (IC50 of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. SMI-4a has anticancer activity[1].

IC₅₀&Target

PIM1 PIM1 PIM2

24 μM (IC50) 0.6 μM (Ki) 100 μM (IC50)

体外研究

Treatment with SMI-4a (0.5 μM; 1 hour; HEK-293T cells) attenuates the autophosphorylation of labeled Pim-1 in intact cells [1].

Western Blot Analysis

Cell Line:

HEK-293T cells

Concentration:

0.5 μM

Incubation Time:

1 hour

Result:

Caused a dose-dependent reduction in Pim-1-induced 4E-BP1 phosphorylation, with an IC₅₀ of approximately 125 nM.

分子式

C₁₁H₆F₃NO₂S

分子量

273.23

CAS号

438190-29-5

中文名称

(5Z)-5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮;Pim1抑制剂SMI-4a

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (365.99 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.6599 mL	18.2996 mL	36.5992 mL
5 mM	0.7320 mL	3.6599 mL	7.3198 mL
10 mM	0.3660 mL	1.8300 mL	3.6599 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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：20% HP-β-CD in saline

Solubility: 5 mg/mL (18.30 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂：0.5% CMC-Na/saline water

Solubility: 2 mg/mL (7.32 mM); Suspended solution; Need ultrasonic

纯度： ≥98%

Data Sheet

SDS

产品使用指南

[1]. Xia Z, et al. Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases. J Med Chem. 2009 Jan 8;52(1):74-86.

The molarity calculator equation

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

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器