| Customization: | Available |
|---|---|
| Powder: | Yes |
| Customized: | Non-Customized |
|
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|
Product Name |
Darolutamide |
|
Purity |
99% |
|
CAS No. |
1297538-32-9 |
|
Molecular Formula |
C19H19ClN6O2 |
|
Molecular Weight |
398.85 |
|
Appearance |
white powder |
|
Shelf life |
24 months under the previously mentioned conditions. |
|
Storage |
Store in a cool dry place, avoiding sunlight directly. |
ODM-201, also known as Darolutamide, is a new-generation, potent and selective androgen receptor (AR) inhibitor which is potential useful for treatment of castration-resistant prostate cancer (CRPC). ODM-201 is a full and high-affinity AR antagonist that, similar to second-generation antiandrogens enzalutamide and ARN-509. Importantly, ODM-201 also blocks the activity of the tested mutant ARs arising in response to antiandrogen therapies, including the F876L mutation that confers resistance to enzalutamide and ARN-509. In addition, ODM-201 reduces the growth of AR-overexpressing VCaP prostate cancer cells both in vitro and in a castration-resistant VCaP xenograft model. ODM-201 overcomes resistance to AR-targeted therapies by antagonizing both overexpressed and mutated ARs. ODM-201 is currently in a phase 3 trial in CRPC.
ODM-201 is a potent and full antagonists for human AR (hAR) with IC50 values of 26 nM by transactivation assays in AR-HEK293 cells.
IC50 value: 26 nM (in AR-HEK293 cells)
Target: androgen receptor
in vitro: ODM-201 is a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies. In competitive AR binding assays, the inhibition constant (Ki) values of ODM-201 were 11 nM.
in vivo: ODM-201 inhibits tumor growth in a castration-resistant VCaP xenograft model in vivo. ODM-201 shows a significant antitumor activity with both doses, 50 mg/kg twice daily being more efficacious compared to castrated, untreated mice (p < 0.001).
Certificate of Analysis
| Batch Number | Z20190412001 | ||
| Production Date | 2019.04.12 | ||
| Batch Quantity | 80 KGS | ||
| Item | Test Standard | Testing Result | |
| Appearance | Powder | Complies | |
| Color | White fine Powder | Complies | |
| Particle Size | 100% pass 80 mesh | Complies | |
| Oder | Characteristic | Complies | |
| Taste | Characteristic | Complies | |
| Loss on Drying | ≤5.0% | 2.20% | |
| Residue on Ignition | ≤0.1% | 0.05% | |
| Residual acetone | ≤0.1% | Complies | |
| Residual Ethanol | ≤0.5% | Complies | |
| Heave Mentals | ≤10ppm | Complies | |
| Na | ≤0.1% | <0.1% | |
| Pb | ≤3 ppm | Complies | |
| Total Plate | <1000CFU/g | Complies | |
| Yeast & Mold | <100 CFU /g | Complies | |
| E. Coli | Negative | Complies | |
| Salmonella | Negative | Complies | |
| Conclusion: Conform with USP Standard | |||
Storage:Closed container. dry & cool. keep away from moisture &strong light
Shelf life:24 Months
Shipping Options as follows
| EMS | Around 7-10 working days |
| DHL | Around 3-5 working days |
| Fedex | Around 4-6 working days |
| TNT | Around 6-7 working days |
| By Air | Around 5-7 working days |
| By Sea | Around 15-30 working days |
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