ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species.
| Molecular Weight | 355.43 |
| CAS Number | 1699720-89-2 |
| 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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