CTCE-9908 

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

CTCE-9908 (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 inhibits ovarian cancer cell migration to CXCL12. CTCE-9908 does not cause apoptosis or cellular senescence, but induces multinucleation, G2-M arrest, and abnormal mitosis in ovarian cancer cells. CTCE-9908 deregulates DNA damage checkpoint proteins and spindle assembly checkpoint proteins at G2-M phases of the cell cycle^[1].

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

CTCE-9908 (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].

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

1927.25

C₈₆H₁₄₇N₂₇O₂₃

1030384-98-5

Solid

White to off-white

Sequence 1:Lys-Gly-Val-Ser-Leu-Ser-Tyr-Arg-Lys-NH2;Sequence 1':Lys-Gly-Val-Ser-Leu-Ser-Tyr-Arg (Amide bridge:Lys9-Arg8’)

Sequence 1:KGVSLSYRK-NH2;Sequence 1':KGVSLSYR (Amide bridge:Lys9-Arg8’)

OC(C=C1)=CC=C1C[C@H](NC([C@H](CO)NC([C@H](CC(C)C)NC([C@H](CO)NC([C@H](C(C)C)NC(CNC([C@@H](N)CCCCN)=O)=O)=O)=O)=O)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(N)=O)CCCCNC([C@H](CCCNC(N)=N)NC([C@@H](NC([C@H](CO)NC([C@H](CC(C)C)NC([C@H](CO)NC([C@H](C(C)C)NC(CNC([C@@H](N)CCCCN)=O)=O)=O)=O)=O)=O)CC2=CC=C(C=C2)O)=O)=O)=O)=O

Room temperature in continental US; may vary elsewhere.

Stored under nitrogen, away from moisture

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

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [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.  [Content Brief]

  [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.  [Content Brief]