2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. SPT-IN-2

SPT-IN-2 是一种口服有效的丝氨酸棕榈酰转移酶 (SPT) 抑制剂 (对人 SPT2 的 IC50=0.71 nM)。SPT-IN-2 可抑制神经酰胺合成、抑制癌细胞生长，并在异种移植小鼠模型中表现出体内抗肿瘤活性、良好的代谢稳定性与细胞膜渗透性。SPT-IN-2 阻断鞘脂从头合成通路，显著降低细胞内神经酰胺含量与 SPT 直接下游产物 3-酮二氢鞘氨醇（3-KDS）的水平。SPT-IN-2 可用于肺腺癌、急性早幼粒细胞白血病、乳腺癌的相关研究。

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SPT-IN-2

SPT-IN-2 Chemical Structure

CAS No. : 2035011-97-1

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规格 价格 是否有货 数量
1 mg ￥2930
13 - 15 周
5 mg 询价 13 - 15 周
10 mg 询价 13 - 15 周
25 mg 询价 13 - 15 周
50 mg   询价  
100 mg   询价  

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SPT-IN-2 相关抗体

Top Publications Citing Use of Products

查看 Acyltransferase 亚型特异性产品:

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ACAT1 ACAT2 MGAT2 ACAT DGAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SPT-IN-2 is an orally active serine palmitoyltransferase (SPT) inhibitor (with an IC50 of 0.71 nM against human SPT2). SPT-IN-2 inhibits ceramide synthesis, suppresses cancer cell growth, and exhibits in vivo anti-tumor activity, favorable metabolic stability and cell membrane permeability in xenograft mouse models. SPT-IN-2 blocks the de novo sphingolipid synthesis pathway, significantly reducing intracellular ceramide levels and the levels of 3-ketodihydrosphingosine (3-KDS), the immediate downstream product of SPT. SPT-IN-2 can be used in research related to lung adenocarcinoma, acute promyelocytic leukemia and breast cancer[1].

体外研究
(In Vitro)

SPT-IN-2 (compound 5) (IC50 4.1 nM； 5 d) 对人急性早幼粒细胞白血病 PL-21 细胞产生强效的增殖抑制作用，95% 置信区间为 3.4-4.7 nM[1]。

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

SPT-IN-2 相关抗体:

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: PL-21 cell
Concentration: 4.1 nM
Incubation Time: 5 days
Result: Exerted potent proliferation-inhibitory effects.
药代动力学
(Parmacokinetics)
Species Dose Route Vdss CLtotal Cmax Tmax AUC MRT F
Mice[1] 0.1 mg/kg i.v. 750 mL/kg 507 mL/h/kg / / / / /
Mice[1] 1 mg/kg p.o. / / 282 ng/mL 1.2 h 1113 ng·h/mL 2.7 h 56 %
体内研究
(In Vivo)

SPT-IN-2 (10 mg/kg、30 mg/kg；灌胃口服给药；Q2D；2 周) 在人急性早幼粒细胞白血病 PL-21 细胞异种移植小鼠模型中展现出显著的体内抗肿瘤活性，可有效抑制异种移植瘤的体内生长，且给药期间未引发小鼠严重体重下降等明显毒副作用[1]。

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

Animal Model: Immunodeficient nude mice bearing human acute promyelocytic leukemia PL-21 cell xenografts
[1]
Dosage: 10 mg/kg and 30 mg/kg
Administration: Oral gavage administration, once every other day (Q2D) for 2 consecutive weeks
Result: Exhibited significant in vivo antitumor efficacy in the PL-21 xenograft mouse model.
Effectively suppressed the growth of xenograft tumors in vivo, and no severe body weight loss or other obvious toxic side effects were observed in the treated mice during the entire administration period.
分子量

542.94

Formula

C26H22ClF3N6O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SPT-IN-2 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SPT-IN-22035011-97-1AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseserine palmitoyltransferasexenograft mouse modelacute promyelocytic leukemiaceramide synthesisbreast cancercancer cell growthlung adenocarcinomaInhibitorinhibitorinhibit

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