Fumitremorgin C (FTC) is a fungal toxin of the diketopiperazines family of compounds. In mammalian cells, FTC is tremorgenic and causes cell cycle arrest. Fumitremorgin C has been shown to reverse resistance to doxorubicin, mitoxantrane, and topotecan in non-Pgp (P-glycoprotein), non-MRP (multidrug resistance protein) multidrug-resistance (MDR) cells. This reversal of resistance is associated with an increase in drug accumulation.
Fumitremorgin C is a specific, selective, and potent inhibitor at micromolar concentrations of the breast cancer resistant protein (BCRP/ABCG2), an ABC transporter associated with chemotherapy resistance. FTC, in combination with mitoxantrone, can be used for the detection of ABCG2 functional activity in several cell lines.
| Molecular Weight | 379.45 |
| Formula | C22H25N3O3 |
| CAS Number | 118974-02-0 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related BCRP/ABCG2/MXR/ABCP Products |
|---|
| CCTA-1523
CCTA-1523 is a potent, selective, reversible, and orally active ABCG2 inhibitor.CCTA-1523 exhibits cytotoxicity and anticancer activity. |
| Ac32Az19
Ac32Az19 is a potent, nontoxic, and highly selective BCRP inhibitor with an EC50 value of 13 nM in BCRP overexpressing HEK293/R2 cells. |
| ML230
ML230 is a selective inhibitor of the ATP-binding transporter subtype ABCG2, and its inhibitory effect on ABCG2 was 36 times that of ABCB1, with EC50 values of 0.13 μM and 4.65 μM, respectively. |
| (S)-ML753286
(S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor that inhibits BCRP efflux transporter protein with an IC50 of 0.6 μM. |
| Efflux inhibitor-1
Efflux inhibitor-1 is a pyrazolo[1,5-a]pyrimidine efflux inhibitor that also selectively targets ABCG2, with IC50s of 0.45 μM and 2.17 μM, respectively. |
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