Bioactivity | OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study[1]. |
Target | 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), 28 nM (rARG1) |
Invitro | OATD-02 在 BMDM 细胞中抑制小鼠 ARG 的IC50 为 912.9 nM,在 CHO-K1 细胞中抑制人 ARG2 的IC50 为 171.6 nM,在人原代肝细胞中抑制 hARG1 的IC50 为 13 mM[1]。 0 --> OATD-02 相关抗体: |
In Vivo | OATD-02 (10 mg/kg, 口服) 在体内具有较强的长效药效,在小鼠、大鼠和犬中的口服生物利用度分别为 13%、30% 和 61%[1]。OATD-02 (5 mg/kg,口服) 在给药结束1周后仍能维持血浆中L -精氨酸浓度增加 4 倍[1]。OATD-02 (每天2次, 50 mg/kg,口服) 可抑制 B16F10 原位异种移植肿瘤的生长[1]。 Animal Model: |
Name | OATD-02 |
CAS | 2146132-73-0 |
Formula | C12H25BN2O4 |
Molar Mass | 272.15 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Borek B, et al. Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy. Mol Cancer Ther. 2023;22(7):807-817. |