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dCBP-1

Cat. No. M25507
dCBP-1 Structure
Size Price Availability Quantity
5mg USD 250  USD250 In stock
10mg USD 420  USD420 In stock
25mg USD 920  USD920 In stock
50mg USD 1480  USD1480 In stock
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Quality Control & Documentation
Biological Activity

dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on Cereblon ligand. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression.

Chemical Information
Molecular Weight 1028.11
Formula C51H63F2N11O10
CAS Number 2484739-25-3
Solubility (25°C) DMSO 30 mg/mL (ultrasonic and warming)
Storage -20°C, protect from light, dry, 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] Whitney K Lieberman, et al. Cell Chem Biol. Chemical control of multidomain acetyltransferase activity

[2] Raghu Vannam, et al. Cell Chem Biol. Targeted degradation of the enhancer lysine acetyltransferases CBP and p300

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