WZH-17-002
WZH-17-002 is a WZH-15-125-based ALK PROTAC degrader with a DC50 of 25 nM. WZH-17-002 enhances activities against Lorlatinib (HY-12215)-resistant ALK compound mutations. WZH-17-002 significantly reduces drug resistance in ALK-fusion non-small cell lung cancer (NSCLC) and inhibits tumor growth in EML4-ALK G1202R/L1196 M xenograft mice model. Pink: ALK ligand (HY-174314); Blue: CRBN ligase ligand (HY-14658); Black: linker (HY-174316)
(Pink: Anaplastic lymphoma kinase (ALK) ligand (HY-174314); Blue: Cereblon ligand (HY-14658); Black: linker (HY-174316)).
For research use only. We do not sell to patients.
- Formula: C47H54BrN11O10S
- Molecular Weight:1044.97
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
| Species | Dose | Route | AUClast | AUC0-∞ | T1/2 | Vss | CL | Cmax | Tmax | F |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat | 1 mg/kg | i.v. | 4279 ng·h/mL | 4317 ng·h/mL | 3.48 h | 0.99 L/kg | 4.19 mL/min/kg | / | / | / |
| Rat | 10 mg/kg | p.o. | 3578 ng·h/mL | 3675 ng·h/mL | 4.07 h | / | / | 269 ng/mL | 4.67 h | 8.5 % |
Chemical Information
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Molecular Weight 1044.97
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Formula C47H54BrN11O10S
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SMILES
O=C(N(CC1)CCN1C(CC2)CCN2C(C(CC)=C3)=CC(OC)=C3NC(N=C4NC5=CC=C6OCCOC6=C5N(S(C)(=O)=O)C)=NC=C4Br)CNC7=C8C(N(C9CCC(NC9=O)=O)C(C8=CC=C7)=O)=O
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
WZH-17-002 Related Classifications
HY-174315 Related Classifications
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