LTX-315(Synonyms: KKWWKKW-Dip-K-NH2)

LTX-315;(Synonyms: KKWWKKW-Dip-K-NH2) 纯度: 99.73%

LTX-315 (KKWWKKW-Dip-K-NH2) 是具有高效抗癌活性的溶瘤肽,抑制 MRC-5,A20 和 AT84 的 IC50 值分别为 34.3, 8.3 和 11 µM。

LTX-315amp;;(Synonyms: KKWWKKW-Dip-K-NH2)

LTX-315 Chemical Structure

CAS No. : 1345407-05-7

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ¥4118 In-stock
2 mg ¥1100 In-stock
5 mg ¥1500 In-stock
10 mg ¥2600 In-stock
25 mg ¥4800 In-stock
50 mg ¥9200 In-stock
100 mg ; 询价 ;
200 mg ; 询价 ;

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LTX-315 相关产品

bull;相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Drug Repurposing Compound Library
  • Peptide Library

生物活性

LTX-315 (KKWWKKW-Dip-K-NH2) is an oncolytic peptide with potent anticancer activity; inhibits MRC-5, A20 and AT84 with IC50s of 34.3, 8.3 and 11 μM, respectively.

IC50 Target

IC50: 34.3 µM (MRC-5), 8.3 µM (A20), 11 µM (AT84)[1]

体外研究
(In Vitro)

LTX-315 is found to be equipotent against drug-resistant cancer cells, nontoxic towards red blood cells, shows high plasma protein binding and is quite rapidly degraded to non-toxic metabolites. LTX-315 induces rapid killing of cancer cells. The oncolytic activity of LTX-315 stems from both a direct lytic effect on the plasma membrane in addition to permeabilization of the mitochondrial membrane, leading to cellular death by necrosis and release of tumor antigens. Treatment of cancer cells with LTX-315 causes the release of several danger signals (DAMPs) that are associated with immunogenic cell death and stimulation of adaptive immune responses[1].

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

体内研究
(In Vivo)

Intratumoral administration of LTX-315 has resulted in complete regression and systemic tumor specific immune responses in several preclinical models[1]. Intratumoral administration of LTX-315 resulted in tumor necrosis and the infiltration of immune cells into the tumor parenchyma followed by complete regression of the tumor in the majority of the animals. LTX-315 induced the release of danger-associated molecular pattern molecules such as the high mobility group box-1 protein in vitro and the subsequent upregulation of proinflammatory cytokines such as interleukin (IL) 1β, IL6 and IL18 in vivo. Animals cured by LTX-315 treatment are protected against a re-challenge with live B16 tumor cells both intradermally and intravenously[2].

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

Clinical Trial

分子量

1439.79

Formula

C78H106N18O9

CAS 号

1345407-05-7

Sequence Shortening

KKWWKKW-{Dip}-K-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

H2O : 100 mg/mL (69.45 mM; Need ultrasonic)

DMSO : ≥ 50 mg/mL (34.73 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 0.6945 mL 3.4727 mL 6.9455 mL
5 mM 0.1389 mL 0.6945 mL 1.3891 mL
10 mM 0.0695 mL 0.3473 mL 0.6945 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:;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.5 mg/mL (1.74 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.74 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (1.74 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.74 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 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
  • 3.

    请依序添加每种溶剂:;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (1.74 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.74 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • [1]. Haug BE, et al. Discovery of a 9-mer Cationic Peptide (LTX-315) as a Potential First in Class Oncolytic Peptide. J Med Chem. 2016 Apr 14;59(7):2918-27.

    [2]. Camilio KA, et al. Complete regression and systemic protective immune responses obtained in B16 melanomas after treatment with LTX-315. Cancer Immunol Immunother. 2014 Jun;63(6):601-13.

Cell Assay
[1]

Tumor cells are incubated for 4 hours with 10 concentrations of LTX-315 in 1/4 dilution step with a top dose of 400 µM, with 1% (final concentration) Triton X-100 as positive control and FBS-free culture medium as negative control. Cell cytotoxicity is measured using the MTS assay[1].

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

Animal Administration
[2]

Mice: Tumor cells are harvested, ished in RPMI-1640 and injected intradermally (i.d.) into the right side of the abdomen in C57BL/6 mice. Palpable tumors are injected i.t. with single doses of LTX-315 or LTX-328 dissolved in saline (1.0 mg peptide/50 μL saline) once a day for 3 consecutive days, and the vehicle control is saline only (0.9% NaCl in sterile water). Tumor size is measured using an electronic caliper[2].

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

参考文献
  • [1]. Haug BE, et al. Discovery of a 9-mer Cationic Peptide (LTX-315) as a Potential First in Class Oncolytic Peptide. J Med Chem. 2016 Apr 14;59(7):2918-27.

    [2]. Camilio KA, et al. Complete regression and systemic protective immune responses obtained in B16 melanomas after treatment with LTX-315. Cancer Immunol Immunother. 2014 Jun;63(6):601-13.