NX-1607 is an oral, small molecule inhibitor of CBL-B with an IC50 of < 1 nM, it has been shown to enhance antigen recall, reduce T cell exhaustion and increase cytokine production upon T cell receptor stimulation, overcoming suppressive signals from the tumor microenvironment (TME). NX-1607 has demonstrated anti-tumor activity and long-term survival in murine models as both a single agent and in combination with programmed cell death protein-1 (PD-1) antibodies. Further, NX-1607 elicits dose-dependent increases in cytokine secretion and proliferation in T-cell receptor-stimulated primary human T cells with enhanced tumor antigen-specific T-cell and NK cell anti-tumor responses.
| Molecular Weight | 537.62 |
| Formula | C30H34F3N5O |
| CAS Number | 2573775-59-2 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage | 4°C, dry, sealed |
| 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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