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Cereblon inhibitor 2

Cat. No. M43410
Cereblon inhibitor 2 Structure
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Biological Activity

Cereblon inhibitor 2 is a Cereblon inhibitor useful in solid tumor research, especially breast cancer.

Chemical Information
Molecular Weight 440.88
Formula C22H21ClN4O4
CAS Number 2639380-62-2
Form Solid
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Shonali Midha et al. Expert Opin Drug Saf. A safety review of recently approved and emerging drugs for patients with relapsed or refractory multiple myeloma

[2] Parva Bhatt et al. Curr Oncol. Relapsed/Refractory Multiple Myeloma: A Review of Available Therapies and Clinical Scenarios Encountered in Myeloma Relapse

[3] Hanrui Jiang et al. Front Chem. E3 ligase ligand optimization of Clinical PROTACs

[4] Xingui Liu et al. J Am Chem Soc. Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable, and Blood-Brain Barrier Penetrant PROTAC Degrader of Leucine-Rich Repeat Kinase 2

[5] Calla M Olson et al. Nat Chem Biol. Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation

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Thalidomide-NH-PEG2-C2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a PEG linker used for dBRD9 synthesis. dBRD9 is a selective BRD9 probe PROTAC degrader for the study of BAF complex biology.
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Thalidomide-O-amido-C4-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker.
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Keywords: Cereblon inhibitor 2 supplier, E3 Ligase Ligand-Linker Conjugates, inhibitors, activators

 
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