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BCRP inhibitor
Mycotoxin. Tremorgenic. Potent and specific inhibitor of the breast cancer resistance protein (BCRP; ABCG2). Reverses multidrug resistance mediated by BCRP and increases cytotoxicity of several anticancer agents in vitro.
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Product Details
| Alternative Name |
FTC, SM-Q |
|---|---|
| Appearance |
White to light brown powder. |
| CAS |
118974-02-0 |
| Couple Target |
BCRP |
| Couple Type |
Inhibitor |
| Formula |
C22H25N3O3 |
| Identity |
Determined by 1H-NMR. |
| MW |
379.5 |
| Purity |
≥96% (HPLC) |
| Solubility |
Soluble in DMSO, methanol or chloroform. |
| Source |
Isolated from Aspergillus fumigatus. |
| Technical Info / Product Notes |
Optical Rotation: [α]D= +19° ±1° (c=1.0 in methanol). |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. |
|---|---|
| Long Term Storage |
+4°C |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- ABC transporter activity linked to radiation resistance and molecular subtype in pediatric medulloblastoma: W.J. Ingram, et al.; Exp. Hematol. Oncol. 2, 26 (2013), Abstract — Full Text
- Cadmium inhibits ABCG2 transporter function in BeWo choriocarcinoma cells and MCF-7 cells overexpressing ABCG2: Kummu, M., Sieppi, E., et al.; Placenta 33, 859 (2012), Abstract
- MDM2 antagonist nutlin-3a reverses mitoxantrone resistance by inhibiting breast cancer resistance protein mediated drug transport: Zhang, F., Throm, S. L., et al.; Biochem. Pharmacol. 82, 24 (2011), Abstract
- Abcg2 overexpression represents a novel mechanism for acquired resistance to the multi-kinase inhibitor Danusertib in BCR-ABL-positive cells in vitro: Balabanov, S., Gontarewicz, A., et al.; PLoS One 6, e19164 (2011), Abstract
- Substrate affinity of photosensitizers derived from chlorophyll-a: the ABCG2 transporter affects the phototoxic response of side population stem cell-like cancer cells to photodynamic therapy: Morgan, J., Jackson, J. D., et al.; Mol. Pharm. 7, 1789 (2010), Abstract
- Estradiol induces export of sphingosine 1-phosphate from breast cancer cells via ABCC1 and ABCG2: K. Takabe, et al.; J. Biol. Chem. 285, 10477 (2010), Abstract
- The beta-carboline alkaloid harmine inhibits BCRP and can reverse resistance to the anticancer drugs mitoxantrone and camptothecin in breast cancer cells: Y. Ma & M. Wink; Phytother. Res. 24, 146 (2010), Abstract
- Role of P-glycoprotein and breast cancer resistance protein-1 in the brain penetration and brain pharmacodynamic activity of the novel phosphatidylinositol 3-kinase inhibitor GDC-0941: L. Salphati, et al.; Drug. Metab. Dispos. 38, 1422 (2010), Abstract
- Histone Deacetylase Inhibitors Induce a Very Broad, Pleiotropic Anticancer Drug Resistance Phenotype in Acute Myeloid Leukemia Cells by Modulation of Multiple ABC Transporter Genes: S. Hauswald, et al.; Clin. Cancer Res. 15, 3705 (2009), Abstract
- ABCG2 expression and side population abundance regulated by a transforming growth factor beta-directed epithelial-mesenchymal transition: Yin, L., Castagnino, P., et al.; Cancer Res. 68, 800 (2008), Abstract
- Plasma pharmacokinetics and tissue distribution of the breast cancer resistance protein (BCRP/ABCG2) inhibitor fumitremorgin C in SCID mice bearing T8 tumors: T.S. Garimella, et al.; Cancer Chemother. Pharmacol. 55, 101 (2005), Abstract
- The role of breast cancer resistance protein in acute lymphoblastic leukemia: S.L. Plasschaert, et al.; Clin. Cancer Res. 9, 5171 (2003), Abstract
- Characterization of drug transport, ATP hydrolysis, and nucleotide trapping by the human ABCG2 multidrug transporter. Modulation of substrate specificity by a point mutation.: Ozvegy, et al.; J. Biol. Chem. 277, 47980 (2002), Abstract
- Fumitremorgin C reverses multidrug resistance in cells transfected with the breast cancer resistance protein.: S.K. Rabindran, et al.; Cancer Res. 60, 47 (2000), Abstract
- Reversal of a novel multidrug resistance mechanism in human colon carcinoma cells by fumitremorgin: S.K. Rabindran, et al.; Cancer Res. 58, 5850 (1998), Abstract
- Novel mammalian cell cycle inhibitors, tryprostatins A, B and other diketopiperazines produced by Aspergillus fumigatus. I. Taxonomy, fermentation, isolation and biological properties: C.B. Cui, et al.; J. Antibiot. 49, 527 (1996), Abstract
- Mycotoxins produced by Aspergillus fumigatus species isolated from molded silage: R.J. Cole, et al.; J. Agric. Food Chem. 25, 826 (1977), Abstract
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