BTX306
BTX306 is a cereblon-targeting molecular glue degrader. BTX306 reduces myeloma cell viability and induces apoptosis. BTX306 overcomes myeloma cell resistance to Lenalidomide (HY-A0003) or Bortezomib (HY-10227). BTX306 is active against primary myeloma cells, and shows efficacy in vivo. BTX306 can be used for myeloma research.
For research use only. We do not sell to patients.
- CAS No.: 2230747-62-1
- Formula: C20H19ClN4O4S
- Molecular Weight:446.91
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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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Biological Activity
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Caspase-3 |
Caspase-8 |
Caspase-9 |
BTX306 (72 h) shows potent anti-proliferation activity against myeloma cell lines with IC50s in the single nanomolar range, including H929, MM1.S, RPMI 8226, and KAS-6/1 cells[1].
BTX306 (1-10 nM, 12 h) induces cleavage of caspase-3, -8, and -9, indicating that it triggers apoptosis in H929, MM1.S, RPMI 8226, and KAS-6/1 cells[1].
BTX306 (0-10 nM, 24 h) rapidly reduces levels of GSPT1, and also of eukaryotic release factor 1 (eRF1), casein kinase 1 α (CK1α), myeloid cell leukemia 1 (MCL-1), and the eukaryotic homolog of the V-Myc avian myelocytomatosis viral oncogene (c-MYC) in MM1.S, MOLP-8, H929, U266, RPMI 8226, and KAS-6/1 cells[1].
BTX306 (0-10 nM) efficiently eliminates human cord blood CD34+ cells while sparing murine hematopoietic cells, and exerts its effects on RPMI 8226 and MM1.S myeloma cell viability in a cereblon-dependent manner, confirming its specificity for human cereblon[1].
BTX306 (0.01-65.61 nM, 3 days) exhibits potent activity against Lenalidomide-resistant, Bortezomib-resistant, and p53 knockout myeloma models in diverse cell lines (including MM1.S, MOLP-8, H929, U266, RPMI 8226, ANBL-6, and KAS-6/1)[1].
BTX306 potently reduces primary myeloma (CD138+ plasma cells) cell viability, and it shows a greater cell viability reduction in MM1.S and KAS-6/1 cells when combined with Bortezomib or Dexamethasone (HY-14648)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H929, MM1.S, RPMI 8226, and KAS-6/1 cells
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Concentration:1, and 10 nM
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Incubation Time:12 h
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Result:Consistently activated cleavage of caspase-3, -8, and -9 at the 10 nM concentration.
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Cell Line:MM1.S, MOLP-8, H929, U266, RPMI 8226, and KAS-6/1 cells
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Concentration:0, 0.01, 0.1, 1, and 10 nM
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Incubation Time:24 h
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Result:Induced Ikaros and Aiolos loss in most cell lines (e.g., MM1.S, H929), but this effect was variable and notably absent in U266 cells.
Reduced eRF1, CK1α, and GSPT expression.
Impacted IRF4 and c-MYC abundance.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NOD-SCID IL2Rγnull mice (6 weeks old) injected with luciferase GFP-transfected MM1.S cells[1]
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Dosage:1, and 10 mg/kg
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Administration:i.p., daily from day7 to day32
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Result:Induced a dose-dependent reduction in myeloma burden by day 32, which was greater in the mice that received the 10.0 mg/kg dose.
Substantially reduced the abundance of CD138+/GFP+ cells at 1.0 mg/kg, while the 10.0mg/kg dose did so completely in one individual mouse.
Chemical Information
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CAS No. 2230747-62-1
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Molecular Weight 446.91
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Formula C20H19ClN4O4S
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SMILES
CC1=CC=C(C=C1Cl)NC(NCC2=C3CN(C(C3=CS2)=O)C4CCC(NC4=O)=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)
BTX306 Related Classifications
HY-177740 Related Classifications
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