CTCE-9908 TFA

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CTCE-9908 TFA 

CTCE-9908 TFA 是一种有效的，选择性的 CXCR4 抑制剂。CTCE-9908 TFA 在表达 CXCR4 的卵巢癌细胞中诱导有丝分裂突变，诱导细胞毒性，抑制迁移。

CTCE-9908 TFA

CTCE-9908 TFA Chemical Structure

规格 是否有货
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CTCE-9908 TFA 的其他形式现货产品:

CTCE-9908

生物活性

CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells[1][2].

IC50 & Target[1]

CXCR4

 

体外研究
(In Vitro)

CTCE-9908 TFA (0-300 μg/mL; for 10 d) inhibits migration and growth in CXCR4-expressing in ovarian cancer cell lines (IGROV, TOV21G and SKOV3). CTCE-9908 TFA inhibits ovarian cancer cell migration to CXCL12. CTCE-9908 TFA does not cause apoptosis or cellular senescence, but induces multinucleation, G2-M arrest, and abnormal mitosis in ovarian cancer cells. CTCE-9908 TFA deregulates DNA damage checkpoint proteins and spindle assembly checkpoint proteins at G2-M phases of the cell cycle[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

CTCE-9908 TFA (25, 50 and 100 mg/kg; s.c.; 5 days per week for 4.5 weeks) alone slows the rate of primary breast tumor growth, with a 45% inhibition of primary tumor growth at 3.5 weeks of treatment with 50 mg/kg in FVB/N TgN (MMTV-PyMT)634 male mice[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

2041.27

Formula

C88H148F3N27O25
Sequence Shortening

Sequence 1:KGVSLSYRK-NH2;Sequence 1′:KGVSLSYR (Amide bridge:Lys9-Arg8’)
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.
Solvent & Solubility
In Vitro: 

H2O

Peptide Solubility and Storage Guidelines:

1.  Calculate the length of the peptide.

2.  Calculate the overall charge of the entire peptide according to the following table:

  Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.  Recommended solution:

Overall charge of peptide Details
Negative (<0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, add NH4OH (<50 μL).
3.  If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.  If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.  Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.  For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献

  • [1]. Joseph Kwong, et al. An antagonist of the chemokine receptor CXCR4 induces mitotic catastrophe in ovarian cancer cells. Mol Cancer Ther. 2009 Jul;8(7):1893-905.

    [2]. Saima Hassan, et al. CXCR4 peptide antagonist inhibits primary breast tumor growth, metastasis and enhances the efficacy of anti-VEGF treatment or docetaxel in a transgenic mouse model. Int J Cancer. 2011 Jul 1;129(1):225-32.

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