CB-5083

Research use only, not for human use.

CB-5083 is a potent, selective, orally bioavailable inhibitor of p97 AAA with IC50 of 11 nM.

CB-5083 is a potent, selective, orally bioavailable inhibitor of p97 AAA with IC50 of 11 nM, specifically targets D2 ATPase site of p97, shows 9.6, 128 and 158-fold less affinity for DNA-PK, mTOR and PIK3C3; causes accumulation of poly-ubiquitinated proteins, retention of ERAD substrates, and generation of irresolvable proteotoxic stress, leading to activation of the apoptotic arm of the unfolded protein response (UPR) in cancer cells; inhibits A549 cell viability with IC50 of 0.67 uM, induces the UPR and apoptosis in xenograft tumor models.Blood Cancer Phase 1 Clinical.

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Animal Model:Nu/Nu nude female mice bearing established human tumor xenografts derived from HCT 116 colon Dosage:75 mg/kg Administration:Administered orally using every day (qd) dosing, for 2 weeks. Result:Showed more profound antitumor activity.

CB5083 | CB 5083

Proteasome/Ubiquitin

p97

p97

Cancer

Blood cancer

1542705-92-9

413.4717

C24H23N5O2

>98% (HPLC)

10 mM in DMSO

O=C(C1=CC=CC2=C1C=C(C)N2C3=NC(NCC4=CC=CC=C4)=C(COCC5)C5=N3)N.

1H-Indole-4-carboxamide, 1-[7,8-dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-

(-20℃)

With Ice Pack

≥ 2 years