Bendamustine hydrochloride (also known as SDX-105) is a DNA-damaging agent with IC50 of 50 μM. Bendamustine displays a distinct pattern of activity unrelated to other DNA-alkylating agents. Bendamustine hydrochloride activates a base excision DNA repair pathway rather than an alkyltransferase DNA repair mechanism. Bendamustine hydrochloride (SDX-105) inhibits mitotic checkpoints and induces mitotic catastrophe. The combination of bendamustine with fludarabine led to a highly synergistic effect in inducing apoptosis, which was 150% higher than expected for bendamustine plus fludarabine. Bendamustine has been used both as sole therapy and in combination with other agents including etoposide, fludarabine, mitoxantrone, methotrexate, prednisone, rituximab and vincristine.
| Molecular Weight | 394.72 |
| Formula | C16H21Cl2N3O2.HCl |
| CAS Number | 3543-75-7 |
| Form | Solid |
| Solubility (25°C) | DMSO 60 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.
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LP-284 is a potent DNA alkylating agent that kills solid tumours. LP-284 can be used in the studies of hematologic cancers with compromised DNA repair, such as mantle cell lymphoma (MCL). |
| 4-Hydroperoxy cyclophosphamide
4-Hydroperoxy cyclophosphamide, the active metabolite form of the precursor Cyclophosphamide, cross-links DNA and induces T-cell apoptosis independent of caspase receptor activation, as well as activating the mitochondrial death pathway through the generation of reactive oxygen species (ROS). It can be used in studies related to rheumatoid arthritis and autoimmune diseases. |
| Diaziquone
Diaziquone is a water-soluble synthetic aziridinyl benzoquinone that selectively alkylates and cross-links DNA, inhibits DNA replication, induces apoptosis, and inhibits the proliferation of tumor cells, with potential antitumor activity. |
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| Methyl methanesulfonate
Methyl methanesulfonate is a SN2-type alkylating agent that primarily methylates the nitrogen atom in purines and has apoptosis-inducing effects. |
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