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THAL-SNS-032

Cat. No. M14876
THAL-SNS-032 Structure
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5mg USD 380  USD380 In stock
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Quality Control & Documentation
Biological Activity

THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).

Chemical Information
Molecular Weight 869.02
CAS Number 2139287-33-3
Solubility (25°C) DMSO 90 mg/mL
Storage -20°C, sealed
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] Mara Del Mar Noblejas-Lpez, et al. Antitumoral Activity of a CDK9 PROTAC Compound in HER2-Positive Breast Cancer

[2] Calla M Olson, et al. Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation

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Keywords: THAL-SNS-032 supplier, PROTAC, inhibitors, activators


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