GMB-805
GMB-805 is a BCR-Abl PROTAC degrader with a DC50 of 30 nM in K562 cells. GMB-805 exerts antiproliferative activity in K562 cells. GMB-805 exhibits potent anti-tumor activity with favorable safety profile in vivo. GMB-805 can be used for chronic myeloid leukemia research.
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- No. CAS: 2489876-41-5
- Fòrmula: C42H46ClF2N9O7S
- Peso molecular:894.39
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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Bcr-Abl 30 nM (DC50) |
GMB-805 (1-30000 nM, 24 h) dose-dependently degrades BCR/Abl protein in K562 cells with a DC50 of 30 nM in K562 cells[1].
GMB-805 (1 μM, 8 h) induces BCR/Abl protein degradation via the proteasome in K562 cells[1].
GMB-805 (1000 nM, 24 h) reduces VHL-dependent BCR/Abl and c-Abl protein levels in K562 cells[1].
GMB-805 (3 days) possesses potent antiproliferative activity against the BCR-Abl driven cell line K562 with an IC50 of 169 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 cells
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Concentration:25, 250 and 2500 nM
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Incubation Time:24 h
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Result:Demonstrated an enhanced ability to induce BCR-Abl degradation.
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Cell Line:K562 cells
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Concentration:1 μM
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Incubation Time:8 h
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Result:Reduced BCR-Abl and Abl protein expression, and this effect was rescued by cotreatment with Epoxomicn (1 μM) (HY-13821).
Reduced BCR-Abl and Abl protein expression, and this effect was not rescued by cotreatment with Chloroquine (50 μM) (HY-17589A).
Reduced BCR-Abl and Abl protein expression, and this effect was rescued by cotreatment with Pevonedistat (1 μM) (HY-70062).
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUClast |
|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 3.67 h | 2.00 h | 536 ng/mL | 2419 ng·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:K562 cells induced-athymic mice[1]
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Dosage:200 mg/kg
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Administration:i.p., once a day for 3 days
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Result:Showed no significant increase in tumor volume.
No toxicity or weight loss was observed in the treated animals.
Chemical Information
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No. CAS 2489876-41-5
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Peso molecular 894.39
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Fòrmula C42H46ClF2N9O7S
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SMILES
O=C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)[C@H](C(C)(C)C)NC(COCCNC4=C(C5=NNC=C5)C=C(C=N4)C(NC6=CC=C(C=C6)OC(F)(F)Cl)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Burslem GM, et al. Scaffold hopping enables direct access to more potent PROTACs with in vivo activity. Chem Commun (Camb). 2020 Jun 23;56(50):6890-6892. [Content Brief]
[2]. Chen X, et al. Mighty mini-PROTACs: an emerging class of degraders. Eur J Med Chem. 2026 Jan 5;301:118202. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GMB-805 Related Classifications
HY-180968 Related Classifications
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