An orally bioavailable inhibitor of p97
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CB-5083

Item No. 19311

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[7,8-dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-1H-indole-4-carboxamide
CAS Number
1542705-92-9
Molecular Formula
C24H23N5O2
Formula Weight
413.5
Purity
≥95%
Formulation
A crystalline solid
λmax
245, 301 nm
SMILES
CC1=CC2=C(C=CC=C2C(N)=O)N1C3=NC(CCOC4)=C4C(NCC5=CC=CC=C5)=N3
InChi Code
InChI=1S/C24H23N5O2/c1-15-12-18-17(22(25)30)8-5-9-21(18)29(15)24-27-20-10-11-31-14-19(20)23(28-24)26-13-16-6-3-2-4-7-16/h2-9,12H,10-11,13-14H2,1H3,(H2,25,30)(H,26,27,28)
InChi Key
RDALZZCKQFLGJP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    CB-5083 is an orally bioavailable inhibitor of p97 (IC50 = 11 nM), a transitional endoplasmic reticulum ATPase also known as valosin-containing protein (VCP).1,2 It disrupts cellular protein homeostasis and demonstrates anti-tumor activity in hematological and solid tumor models. CB-5083 causes accumulation of poly-ubiquitinated proteins, retention of endoplasmic reticulum-associated degradation (ERAD) substrates, and activation of the apoptotic arm of the unfolded protein response.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Anderson, D.J., Le Moigne, R., Dkjakovic, S., et al. Targeting the AAA ATPase p97 as an Approach to Treat Cancer through Disruption of Protein Homeostasis. Cancer Cell. 28(5), 653-665 (2015).

    2. Zhou, H.-J., Wang, J., Yao, B., et al. Discovery of a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 AAA ATPase (CB-5083). J. Med. Chem. 58(24), 9480-9497 (2015).