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dBET6

Cat. No. M9238
dBET6 Structure
Size Price Availability Quantity
5mg USD 150 In stock
10mg USD 250 In stock
25mg USD 480 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

dBET6 is a highly potent, selective and cell-permeable degrader of BET, which has antitumor activity. dBET6 (100 nM) exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines via degradation of BRD4.

In vivo, dBET6 (7.5 mg/kg, p.o., BID) reduces the leukemic burden in a disseminated mouse model of T-ALL.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 841.37
Formula C42H45ClN8O7S
CAS Number 1950634-92-0
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment.
Winter GE, et al. Mol Cell. 2017 Jul 6;67(1):5-18.e19. PMID: 28673542.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: dBET6 supplier, Epigenetic Reader Domain, inhibitors

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