Microtubule inhibitor
Plant alkaloid that arrests the cell cycle in G2/M phase by blocking mitotic spindle formation. Depolymerizes microtubules and blocks binding of tubulin to microtubule proteins. Causes aberrant tubulin polymerization. Induces apoptosis. Triggers Raf-1 activation, phosphorylation of Bcl-2 family proteins and induction of p53 expression. Cancer chemotherapeutic agent. Posttranscriptionally downregulates HIF-1α expression.
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Product Details
Alternative Name |
VCR . sulfate, Leukocristine . sulfate |
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Appearance |
White to off-white powder. |
CAS |
2068-78-2 |
Couple Target |
HIF, Microtubule |
Couple Type |
Inhibitor |
Formula |
C46H56N4O10 . H2SO4 |
MI |
14: 9986 |
MW |
825.0 . 98.1 |
Purity |
≥98% TLC |
RTECS |
OH6340000 |
Solubility |
Soluble in water (25mg/ml) or methanol. |
Technical Info / Product Notes |
Note: Product is not sterile. |
Handling & Storage
Use/Stability |
As indicated on product label or CoA when stored as recommended. Stable for at least 1 year after receipt when stored at -20°C. Stock solutions are stable for up to 3 months at -20°C. |
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Handling |
Protect from light and moisture. |
Long Term Storage |
-20°C |
Shipping |
Ambient Temperature |
Regulatory Status |
RUO – Research Use Only |
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- Low-dose Pimecrolimus, an FDA-approved Calcineurin Inhibitor, Sensitizes Drug-resistant Cancer Cells via Strong P-gp Inhibition: J.H. Park, et al.; Anticancer Res. 43, 1103 (2023), Abstract
- Combination Treatment Using Pyruvate Kinase M2 Inhibitors for the Sensitization of High Density Triple-negative Breast Cancer Cells: J.S. Lee, et al.; In Vivo 36, 2105 (2022), Abstract
- PKM2 Is Overexpressed in Glioma Tissues, and Its Inhibition Highly Increases Late Apoptosis in U87MG Cells With Low-density Specificity: J.H. Park, et al.; In Vivo 36, 694 (2022), Abstract
- Drug Screening of Primary Patient Derived Tumor Xenografts in Zebrafish: Haney, M. G., Moore, L. H., et al.; J. Vis. Exp. , (2020), Abstract
- Novel SIRT1 inhibitor 15-deoxy-Δ12,14-prostaglandin J2 and its derivatives exhibit anticancer activity through apoptotic or autophagic cell death pathways in SKOV3 cells: Tae, I. H., Park, E. Y., et al.; Int. J. Oncol. 53, 2518 (2018), Abstract
- Co-treatment with Celecoxib or NS398 Strongly Sensitizes Resistant Cancer Cells to Antimitotic Drugs Independent of P-gp Inhibition: J.S. Lim, et al.; Anticancer Res. 36, 5063 (2016), Application(s): Cell Treatment, Abstract — Full Text
- Selenate specifically sensitizes drug-resistant cancer cells by increasing apoptosis via G2 phase cell cycle arrest without P-GP inhibition: A.R. Choi, et al.; Eur. J. Pharmacol. 764, 63 (2015), Application(s): Cell Culture, Abstract
- 2ME2 inhibits tumor growth and angiogenesis by disrupting microtubules and dysregulating HIF: N.J. Mabjeesh, et al.; Cancer Cell 3, 363 (2003), Abstract
- Selective toxicity of vincristine against chronic lymphocytic leukemia cells in vitro: J.A. Vilpo, et al.; Eur. J. Haematol. 65, 370 (2000), Abstract
- Vincristine-induced apoptosis in vivo in peripheral blood mononuclear cells of children with acute lymphoblastic leukaemia (ALL): E. Groninger, et al.; Br. J. Haematol. 111, 875 (2000), Abstract
- The effect of antimicrotubule agents on signal transduction pathways of apoptosis: a review: L.G. Wang, et al.; Cancer Chemother. Pharmacol. 44, 355 (1999), (Review), Abstract
- Tubulin as a target for anticancer drugs: agents which interact with the mitotic spindle: A. Jordan, et al.; Med. Res. Rev. 18, 259 (1998), Abstract
- Bcl-xL is phosphorylated in malignant cells following microtubule disruption: M.S. Poruchynsky, et al.; Cancer Res. 58, 3331 (1998), Abstract
- Raf-1/bcl-2 phosphorylation: a step from microtubule damage to cell death: M.V. Blagosklonny, et al.; Cancer Res. 57, 130 (1997), Abstract
- Antimitotic natural products and their interactions with tubulin: E. Hamel; Med. Res. Rev. 16, 207 (1996), Abstract
- Bcl-2 interrupts the ceramide-mediated pathway of cell death: J. Zhang, et al.; PNAS 93, 5325 (1996), Abstract
- Interaction of vinca alkaloids with tubulin: a comparison of vinblastine, vincristine, and vinorelbine: S. Lobert, et al.; Biochemistry 35, 6806 (1996), Abstract
- Cell death induced by vincristine in the intestinal crypts of mice and in a human Burkitt’s lymphoma cell line: B.V. Harmon, et al.; Cell Prolif. 25, 523 (1992), Abstract
- Binding selectivity of rhizoxin, phomopsin A, vinblastine, and ansamitocin P-3 to fungal tubulins: differential interactions of these antimitotic agents with brain and fungal tubulins [published erratum appears in BBRC 190, 1180 (1993)]: Y. Li, et al.; BBRC 187, 722 (1992), Abstract
- Interactions of the catharanthus (Vinca) alkaloids with tubulin and microtubules: R.H. Himes; Pharmacol. Ther. 51, 257 (1991), Abstract
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