Analog of the fungal toxin fumitremorgin C (Prod. No. ALX-350-127). Potent and selective inhibitor of the breast cancer resistance protein multidrug transporter (BCRP, EC90=26nM). Highly effective for increasing the intracellular drug accumulation and reversing BCRP-mediated multidrug resistance yet has little activity against P-glycoprotein, multidrug resistance-associated protein (MRP1) and other known drug transporters. In mouse models Ko143 was able to restore the intracellular accumulation and abolish the directionality in net flux of dasatinib. It is a highly useful tool for the identification of drug transport processes in complex experimental systems.
Product Details
| Alternative Name: | (3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxopyrazino-[1',2':1,6]pyrido[3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester |
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| Formula: | C26H35N3O5 |
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| MW: | 469.6 |
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| CAS: | 461054-93-3 |
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| Purity: | ≥96% (HPLC) |
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| Appearance: | White solid. |
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| Solubility: | Soluble in DMSO (>25mg/ml) or 100% ethanol (>25mg/ml). |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Store solutions at -20°C for up to 3 months. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
ABCB1 as a potential beneficial target of midostaurin in acute myeloid leukemia: S. Sucha, et al.; Biomed. Pharmacother.
150, 112962 (2022),
Abstract;
Folium Sennae Increased the Bioavailability of Methotrexate through Modulation on MRP 2 and BCRP: C.P. Yu, et al.; Pharmaceuticals
14, 1036 (2021),
Abstract;
Increased Systemic Exposure of Methotrexate by a Polyphenol-Rich Herb via Modulation on Efflux Transporters Multidrug Resistance-Associated Protein 2 and Breast Cancer Resistance Protein: C.P. Yu, et al.; J. Pharm. Sci.
105, 343 (2016),
Application(s): Positive inhibitor of BCRP,
Abstract;
Dinaciclib, a cyclin-dependent kinase inhibitor, is a substrate of human ABCB1 and ABCG2 and an inhibitor of human ABCC1 in vitro: D. Cihalova, et al.; Biochem. Pharmacol.
98, 465 (2015),
Application(s): MDCKII monolayer transport assay,
Abstract;
Influence of drug transporters and stereoselectivity on the brain penetration of pioglitazone as a potential medicine against Alzheimer's disease: K.L. Chang, et al.; Sci. Rep.
5, 9000 (2015),
Application(s): Cell Culture,
Abstract;
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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
Identification of novel specific and general inhibitors of the three major human ATP-binding cassette transporters P-gp, BCRP and MRP2 among registered drugs: P. Matsson, et al.; Pharm. Res.
26, 1816 (2009),
Abstract;
P-glycoprotein and breast cancer resistance protein influence brain distribution of dasatinib: Y. Chen, et al.; J. Pharmacol. Exp. Ther.
330, 956 (2009),
Abstract;
Potent and specific inhibition of the breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C: J.D. Allen, et al.; Mol. Cancer Ther.
1, 417 (2002),
Abstract;
