OATD-02
Based on 1 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 2146132-73-0
- Formula: C12H25BN2O4
- Molecular Weight:272.15
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) OATD-02
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Biological Activity
20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), 28 nM (rARG1)
OATD-02 inhibits mouse ARG in BMDM cells with IC50 values of 912.9 nM and human ARG2 in transfected CHO-K1 cells with IC50 of 171.6 nM, and inhibits hARG1 in human primary hepatocytes at a much higher micromolar concentration (IC50 = 13 μM) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
OATD-02 (5 mg/kg, oral gavage) increases fourfold of the L-arginine concentration in plasma sustained even 1 week after end of a treatment[1].
OATD-02 (twice per day at 50 mg/kg, oral gavage) inhibits the tumor growth in B16F10 orthotopic xenograft tumor model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B16F10 orthotopic xenograft tumor model[1]
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Dosage:Twice per day at 50 mg/kg for 15days
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Administration:Oral gavage
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Result:Inhibited tumor growth (TGI 46%).
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2146132-73-0
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Molecular Weight 272.15
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Formula C12H25BN2O4
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SMILES
N[C@]1(C(O)=O)C[C@H](CCB(O)O)CC[C@H]1CN(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Blockade of CCR5+ T Cell Accumulation in the Tumor Microenvironment Optimizes Anti-TGF-β/PD-L1 Bispecific Antibody. [Abstract]2024 Sep 20:e2408598. PMID: 39303165
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)