(Rac)-Nutlin-3


CAS No. : 890090-75-2

(Synonyms: (Rac)-Rebemadlin)

890090-75-2
Price and Availability of CAS No. : 890090-75-2
Size Price Stock
100 mg Get quote
250 mg Get quote
500 mg Get quote
We match the lowest price on market.

We offer a substantial discount on larger orders, please inquire via [email protected]

or Fax: (86)21-58955996

Inquiry for price and availability only. Please place your order via our email or fax.

Cat. No. : HY-10029A
M.Wt: 581.49
Formula: C30H30Cl2N4O4
Purity: >98 %
Solubility: 10 mM in DMSO;10 mM in DMSO
Introduction of 890090-75-2 :

(Rac)-Nutlin-3 (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). (Rac)-Nutlin-3 inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. (Rac)-Nutlin-3 has the potential for the study of TP53 wild-type ovarian carcinomas[1][2]. In Vitro:Nutlin-3a is a therapeutic which inhibits MDM2, activates wild-type p53, and induces apoptosis-as a therapeutic compound for TP53 wild-type ovarian carcinomas. Three cell lines (HOC-7, OVCA429 and A2780) with wild-type TP53 are highly sensitive to Nutlin-3a (IC50=4 to 6 μM). SKOV3 cells have an IC50 of 38 μM to Nutlin-3a. The two remaining ovarian clear cell lines (TOV21G and OVAS), both with TP53 wild-type, are relatively more sensitive to growth inhibition with Nutlin-3a (IC50=14 and 25 μm respectively) than the TP53 mutant cell lines[1]. Nutlin-3a is the active enantiomer of Nutlin-3. Nutlin-3a is a highly selective MDM2 antagonist and p53 inducer. Seven days of incubation with 10 μM Nutlin-3a leads to >90% inhibition of NIH/3T3 cells’growth but does not affect the proliferation of MEF in which both targets of the drug are eliminated. Nutlin-3a effectively arrestes cell-cycle progression in all cell lines, depleting the S-phase compartment to 0.2-2% and increasing the G1- and G2/M-phase compartments, indicating G1 and G2 arrest. The p53 targets p21 and MDM2 are elevated significantly 3 h after Nutlin-3a addition and reach maximal levels at 8 h. Nutlin-3a induces apoptosis in ≈60% of SJSA-1 and MHM cells after 40 h, which increase further after 60 h (85% and 65%, respectively)[2]. In Vivo:Nutlin-3a is efficacious in all models with average tumor growth inhibition ≥98%. Nutlin-3a suppresses xenograft growth in a dose-dependent fashion with the highest dose (200 mg/kg) showing a substantial tumor shrinkage (eight partial and one full regressions). The established SJSA-1 and MHM osteosarcoma xenografts with Nutlin-3a causes extensive tumor regression[2].

Your information is safe with us.