2. GPCR/G Protein Immunology/Inflammation
  3. CXCR
  4. Motixafortide

Motixafortide  (Synonyms: BKT140 (4-fluorobenzoyl); BL-8040; TF14016)

目录号: HY-P0171 纯度: 99.88%
COA 产品使用指南

摩尔计算器

Motixafortide (BKT140 4-fluorobenzoyl) 是一种新型的CXCR4拮抗剂，IC50约为1 nM。

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Custom Peptide Synthesis

Motixafortide Chemical Structure

Motixafortide Chemical Structure

CAS No. : 664334-36-5

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规格 价格 是否有货 数量
5 mg ￥2800
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10 mg ￥4500
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25 mg ￥9000
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Motixafortide 相关抗体

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ～1 nM.

IC50 & Target[1]

CXCR4

~1 nM (IC50)

体外研究
(In Vitro)

Motixafortide (BKT140) displays selective toxicity toward AmL and MM cells. Treatment with Motixafortide (BKT140) can overcome IL-6 dependent proliferation and survival of ARH77 MM cells. Motixafortide (BKT140) specifically triggers CXCR4-dependent cell death in leukemia and MM cells. Motixafortide (BKT140) stimulates apoptotic cell death in leukemia and MM cells[2].

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

Motixafortide 相关抗体:
体内研究
(In Vivo)

Subcutaneous injections of Motixafortide (BKT140) significantly reduces, in a dose-dependent manner, the growth of human acute myeloid leukemia and multiple myeloma xenografts. Tumors from animals treated with Motixafortide (BKT140) are smaller in size and weights, had larger necrotic areas and high apoptotic scores[2].

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

2159.52

Formula

C97H144FN33O19S2
CAS 号
性状

固体

颜色

White to off-white

Sequence

{4-Fluorobenzoyl}-Arg-Arg-{2-Naph-Ala}-Cys-Tyr-{Cit}-Lys-{d-Lys}-Pro-Tyr-Arg-{Cit}-Cys-Arg-NH2 (Disulfide bridge: Cys4-Cys13)
Sequence Shortening

{4-Fluorobenzoyl}-RR-{2-Naph-Ala}-CY-{Cit}-K-{d-Lys}-PYR-{Cit}-CR-NH2 (Disulfide bridge: Cys4-Cys13)
运输条件

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

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 100 mg/mL (46.31 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H2O 中的溶解度 : 50 mg/mL (23.15 mM; 超声助溶)

* "≥" 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 0.4631 mL 2.3153 mL 4.6307 mL
5 mM 0.0926 mL 0.4631 mL 0.9261 mL
查看完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

以下溶解方案，请直接配置工作液。建议现用现配，在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂： PBS

    Solubility: 110 mg/mL (50.94 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.88%

COA (207 KB) RP-HPLC (200 KB) 元素分析报告 (224 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[2]

Hematopoietic cancer cells are incubated with different concentrations of Motixafortide (BKT140) or AMD3100 for 24 hours. Motixafortide (BKT140) is treated with 1M hydrochloric acid (HCL) to achieve a pH of 2.7 to 3 at room temperature for 30 minutes and the pH is adjusted to 7 using concentrated NaOH. Proteinase K is added to Motixafortide (BKT140) at a final concentration of 100 mg/mL, incubated at 37°C for 1 hour, and inactivated by heat treatment (65°C for 30 minutes). After incubation, cells are stained with propidium iodide and the percent of viable PI-negative cells in culture is determined[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice: Severe combined immune-deficient (SCID)/beige mice (C.B-17/IcrHsd-SCID-bg) are used in the study. NB4 cells resuspended in PBS are injected subcutaneously into the flanks of the mice (200 μL per mouse containing 5×106 cells). Tumor growth is monitored daily, and mice are randomized to drug-treated or control PBS-treated groups (10 mice per group) when the tumor size (width×length) reaches 0.04 cm2. BKT140 is administered subcutaneously at a dose of 200 μg per mouse each day for 5 days[2].

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

Motixafortide 相关分类

完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 0.4631 mL 2.3153 mL 4.6307 mL 11.5766 mL
5 mM 0.0926 mL 0.4631 mL 0.9261 mL 2.3153 mL
10 mM 0.0463 mL 0.2315 mL 0.4631 mL 1.1577 mL
15 mM 0.0309 mL 0.1544 mL 0.3087 mL 0.7718 mL
20 mM 0.0232 mL 0.1158 mL 0.2315 mL 0.5788 mL
DMSO 25 mM 0.0185 mL 0.0926 mL 0.1852 mL 0.4631 mL
30 mM 0.0154 mL 0.0772 mL 0.1544 mL 0.3859 mL
40 mM 0.0116 mL 0.0579 mL 0.1158 mL 0.2894 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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:

Motixafortide664334-36-5BKT140 (4-fluorobenzoyl) BL-8040 TF14016BL8040BL 8040BL-8040TF14016TF 14016TF-14016CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsInhibitorinhibitorinhibit

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