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  1. Protein Tyrosine Kinase/RTK Apoptosis
  2. IGF-1R Apoptosis
  3. Dalotuzumab

Dalotuzumab  (Synonyms: 達(dá)羅托組單抗; MK-0646; h7C10)

目錄號: HY-P99284 純度: 97.43%
COA

Dalotuzumab (MK-0646) 是一種靶向 IGF-1R 的重組人源化單克隆抗體 (IgG1 型)。Dalotuzumab 通過抑制 IGF-1IGF-2 介導(dǎo)的腫瘤細(xì)胞增殖、IGF-1R 自體磷酸化和 Akt 磷酸化而發(fā)揮作用。Dalotuzumab 還可誘導(dǎo)細(xì)胞凋亡和周期停滯。Dalotuzumab 與其他抗癌活性分子(如他汀類活性分子)共同使用,可增強(qiáng) Dalotuzumab 的體外和體內(nèi)抗腫瘤活性。

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CAS No. : 1005389-60-5

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Dalotuzumab (MK-0646) is a recombinant humanized monoclonal antibody (IgG1 type) targeting IGF-1R. Dalotuzumab acts by inhibiting IGF-1- and IGF-2-mediated tumor cell proliferation, IGF-1R autophosphorylation, and Akt phosphorylation. Dalotuzumab also induces apoptosis and cycle arrest. Dalotuzumab in combination with other anticancer agents such as statins can enhance the antitumor activity of Dalotuzumab in vitro and in vivo[1][2][3].

同型

Human IgG1 kappa

推薦同型對照抗體
種屬

Humanized

體外研究
(In Vitro)

Dalotuzumab (h7C10; 33 nM; 24 h) 抑制 IGF-1 和 IGF-2 誘導(dǎo)的 MCF7 雌激素依賴性乳腺癌細(xì)胞增殖,IC50 值分別為 4.2 和 3.1 nM[1]。
Dalotuzumab (33 nM; 24 h) 在 IGF-1 誘導(dǎo)的 MCF7 細(xì)胞中,誘導(dǎo)周期停滯,并抑制 IGF-IR 和 IRS-1 的自磷酸化[1]
Dalotuzumab 使 NK 細(xì)胞介導(dǎo)的 MCF7 和 A459 細(xì)胞的裂解率分別提高了 26% 和 25%[1]。
Dalotuzumab (MK-0646; 10 μg/mL; 24, 48 h) 消除 IGF1 在子宮內(nèi)膜癌細(xì)胞中的抗凋亡作用[2]。

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

Cell Proliferation Assay[1]

Cell Line: MCF7 cells (IGF-1 and IGF-2-induced)
Concentration: 33 nM
Incubation Time: 24 h
Result: Showed anti-proliferation activity to IGF-1- and IGF-2-induced MCF7, with IC50 values of 4.2 and 3.1 nM, respectively.

Cell Cycle Analysis[1]

Cell Line: MCF7 cells (IGF-1-induced)
Concentration: 33 nM
Incubation Time: 24 h
Result: Prevented cell cycle progression from the G1 to S and G2/M phases.

Apoptosis Analysis[2]

Cell Line: ECC-1 and USPC-1 cells (IGF-1-induced)
Concentration: 10 μg/mL
Incubation Time: 24, 48 h
Result: Reversed the effect of IGF1 on caspase-3 cleavage (Caspase-3 is activated in apoptotic cells and cleaves several cellular proteins, including PARP).

Western Blot Analysis[1]

Cell Line: MCF7 cells (IGF-1-induced)
Concentration: 33 nM
Incubation Time: 24 h
Result: Led to a decrease of phosphorylation for both β-chain and IRS-1.
體內(nèi)研究
(In Vivo)

Dalotuzumab (h7C10; i.p.; 第一次 250 μg/小鼠,然后每周兩次 125 μg/小鼠,持續(xù) 40 天) 顯示對 MCF-7 和 A549 異種移植腫瘤模型的抗腫瘤作用[1]

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

Animal Model: Swiss Nude mice (MCF-7 and A549 xenograft tumor models)[1].
Dosage: 125 and 250 (first time) μg/mice
Administration: Intraperitoneal injection; 250 μg/mice for the first time, then 125 μg/mice twice weekly for 40 days
Result: Led to average tumor volume at 6 weeks post-cell injection was reduced by 70% and 72% in the MCF-7 and A549 models, respectively.
Clinical Trial
分子量

146.4 (kDa)

CAS 號
性狀

液體

顏色

Colorless to light yellow

中文名稱

達(dá)羅托組單抗

運(yùn)輸條件

Shipping with dry ice.

儲(chǔ)存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

Format
  • Human IgG1 kappa
Biological Activity
  • Immobilized Human IGF1R Protein (ECD, His Tag) can bind Dalotuzumab. The EC50 for this effect is 0.98 ng/mL.
純度 & 產(chǎn)品資料
參考文獻(xiàn)
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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.

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產(chǎn)品名稱:
Dalotuzumab
目錄號:
HY-P99284
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