产品描述
MBC-11 trisodium has potential to treat tumor-induced bone disease (TIBD).It is a first-in-class conjugate of the bone-targeting bisphosphonate HEDP covalently linked to the antimetabolite Ara-C.
体外活性
MBC-11 decreases KAS-6/1 cell growth from approximately 56% at 10-8 M to 6% at 10-5 M[1].MBC-11 shows similar activity profiles and significantly inhibits growth of all three cell lines between 10-8 and 10-4 M.
体内活性
These results demonstrate that MBC-11 decreases bone tumor burden, maintains bone structure, and may increase overall survival, warranting further investigation as a treatment for tumor-induced bone disease (TIBD)[1].MBC-11 (0.04 μg/day, s.c.) has a lower incidence of bone metastases of 40% compared to those treated with PBS (90%) or 0.04 μg/day zoledronate (100%).?MBC-11 also significantly decreases bone tumor burden compared to PBS- or zoledronate-treated mice[1].?Weight gained in mice treated with up to 500 μg/day of MBC-11 is similar to the PBS treated group[1].
Cas No.
387877-45-4
分子式
C11H20N3NaO14P3
分子量
534.2
储存和溶解度
H2O:125 mg/mL (216.58 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years