2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Bcr-Abl
  4. 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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GMB-805

GMB-805 Chemical Structure

CAS No. : 2489876-41-5

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GMB-805 Related Antibodies

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Description

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[1][2].

IC50 & Target[1]

Bcr-Abl

30 nM (DC50)

In Vitro

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.

GMB-805 Related Antibodies

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 25, 250 and 2500 nM
Incubation Time: 24 h
Result: Demonstrated an enhanced ability to induce BCR-Abl degradation.

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 1 μM
Incubation Time: 8 h
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).
Parmacokinetics
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
In Vivo

GMB-805 (200 mg/kg, i.p., once a day for 3 days) exhibits potent anti-tumor activity with favorable safety profile in a K562 xenograft mouse model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: K562 cells induced-athymic mice[1]
Dosage: 200 mg/kg
Administration: i.p., once a day for 3 days
Result: Showed no significant increase in tumor volume.
No toxicity or weight loss was observed in the treated animals.
Molecular Weight

894.39

Formula

C42H46ClF2N9O7S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GMB-805 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GMB-8052489876-41-5GMB805GMB 805PROTACsBcr-AblPROTACK562 cellssafety profileChronic Myeloid LeukemiaInhibitorinhibitorinhibit

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