Combretastatin A4 (CA-4; CRC 87-09)

Alias: Combretastatin A-4; Combretastatin A4; CRC 87-09;Combretastatin A 4;CA-4;CRC 87-09;CA4;CRC 87-09; CA 4;
Cat No.:V1610 Purity: ≥98%
Combretastatin A4 (CA-4; CRC-87-09; Combretastatin A-4) is a highly potent tubulin/microtubuleinhibitor or microtubule polymerization destablizer with potential antitumor activity.
Combretastatin A4 (CA-4; CRC 87-09) Chemical Structure CAS No.: 117048-59-6
Product category: Microtubule Associated
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Combretastatin A4 (CA-4; CRC-87-09; Combretastatin A-4) is a highly potent tubulin/microtubule inhibitor or microtubule polymerization destablizer with potential antitumor activity. It belongs to the so called microtubule-targeting agent (MTA) or microtubule disrupting agent and acts by binding to β-tubulin with a Kd of 0.4 μM. It has been in clinical trials for treating various cancers.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Forward scatter is greatly reduced and the proportion of Annexin-V bound cells is significantly increased when combretastatin A4 phosphate (≥ 50 μM) is used. The amount of hemolysis is not considerably increased by combretastatin A4 phosphate. Combretastatin A4 phosphate at concentrations of several hundred μM markedly increased Fluo3 fluorescence. When extracellular Ca2+ is removed, the effect of Combretastatin A4 phosphate (100 μM) on Annexin-V binding is greatly reduced but not completely eliminated. ROS and ceramide are not significantly increased by combretastatin A4 phosphate (≥ 50 μM), but it does dramatically lower GSH abundance and ATP levels [2]. Strong synergistic cytotoxicity was demonstrated by polymer capsules co-encapsulating doxorubicin-combretastatin-A4 phosphate (1:10) against human nasopharyngeal epithelial carcinoma (KB) cells [3]. The expression of these important molecules and the quantity of VM in 3-D cells are unaffected by pretreatment with combretastatin A4 phosphate [4].
ln Vivo
Thirty minutes after the treatment, rats given 120 mg/10 mL/kg of Combretastatin A4 disodium phosphate had more DBP and MBP. Rats treated with Combretastatin A4 disodium phosphate 120 mg/10 mL/kg showed the following toxicokinetic characteristics for both Combretastatin A4 and its phosphate: Cmax, T1/2, and AUC0-inf values of Combretastatin A4 were 156± 13 μM, 5.87±1.69 h, and 89.4±10.1 h·μM[1]. W256 tumors showed a substantial intratumoral hypoxia following combretastatin A4 phosphate therapy, which was associated by an increase in VM development. Tumor growth was delayed with cercopetastatin A4 phosphate for a mere two days, however the growth of the tumor quickly resumed. Positive correlations were seen between the VM density and the tumor weight and volume on day 8. Through the HIF-1α/EphA2/PI3K/matrix metalloproteinase (MMP) signaling pathway, cercetastatin A4 phosphate stimulates hypoxia and VM formation in W256 tumors, which impairs tumor renewal [4].
Animal Protocol
Dissolved in DMSO; 100 mg/kg; i.p. injection
FVB/N or nude NMRI female mice bearing NT2 and MDA-MB-231 tumors
References
[1]. Tochinai R, et al. Combretastatin A4 disodium phosphate-induced myocardial injury. J Toxicol Pathol. 2016 Jul;29(3):163-71.
[2]. Signoretto E, et al. Stimulation of Eryptosis by Combretastatin A4 Phosphate Disodium (CA4P). Cell Physiol Biochem. 2016;38(3):969-8
[3]. Zhu J, et al. Co-Encapsulation of Combretastatin-A4 Phosphate and Doxorubicin in Polymersomes for Synergistic Therapy of Nasopharyngeal Epidermal Carcinoma. J Biomed Nanotechnol. 2015 Jun;11(6):997-1006.
[4]. Yao N, et al. Combretastatin A4 phosphate treatment induces vasculogenic mimicry formation of W256 breast carcinoma tumor in vitro and in vivo. Tumour Biol. 2015 Nov;36(11):8499-510
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H20O5
Molecular Weight
316.35
CAS #
117048-59-6
SMILES
O(C([H])([H])[H])C1C(=C([H])C(/C(/[H])=C(/[H])\C2C([H])=C([H])C(=C(C=2[H])O[H])OC([H])([H])[H])=C([H])C=1OC([H])([H])[H])OC([H])([H])[H]
Synonyms
Combretastatin A-4; Combretastatin A4; CRC 87-09;Combretastatin A 4;CA-4;CRC 87-09;CA4;CRC 87-09; CA 4;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 63 mg/mL (199.1 mM)
Water:<1 mg/mL
Ethanol:34 mg/mL (107.5 mM)
Solubility (In Vivo)
5%DMSO+50%PEG 300+ddH2O: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.1611 mL 15.8053 mL 31.6106 mL
5 mM 0.6322 mL 3.1611 mL 6.3221 mL
10 mM 0.3161 mL 1.5805 mL 3.1611 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • Combretastatin A4

    Effects of CA-4 and 4h on interphase microtubules. J Med Chem. 2014 Apr 24;57(8):3369-81.
  • Combretastatin A4
    Flow cytometric analysis of cell cycle distributions of HeLa cells treated with pyridine-bridged CA-4 analogues 4h and 4s. J Med Chem. 2014 Apr 24;57(8):3369-81.
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