Navitoclax [923564-51-6]

Catalog number: HY-10087_100mg
Brand: MedChem Express
Packing: 100 mg
Other sizes: 5 mg
10 mg
10 mM
25 mg
50 mg
Price: € 278.00
Expected delivery time: 10 days
Navitoclax Chemical Structure
CAS No. : 923564-51-6...

Product specifications for - Navitoclax [923564-51-6]

Product group: Chemicals
Category: Other
CAS No.: 923564-51-6
Purity: >98%
Molecular Formula: C47H55ClF3N5O6S3
Molecular weight: 974.61
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of <= 0.5 nM, <=1 nM and <=1 nM. IC50 Value: <= 0.5 nM(Ki for Bcl-xL), <=1 nM(Ki for Bcl-2), <=1 nM(Ki for Bcl-w) Target: Bcl-2 Family in vitro: ABT-263 displays the protection afforded by overexpression of Bcl-2 or Bcl-xL with EC50 values of 60 nM and 20 nM, respectively. A wide range of cellular activity is observed with ABT-263 having a 50% growth inhibition (EC50) of 110 nM against the most sensitive line (H146), whereas its activity in the least sensitive line (H82) results in an EC50 at 22 uM. All four cell lines with EC50 values of <400 nM (H146, H889, H1963, and H1417) are also highly sensitive to ABT-737, and the two most resistant lines (H1048 and H82) are similarly resistant to ABT-263. in vivo: ABT-263 is administered at 100 mg/kg/day in the H345 xenograft model, significant antitumor efficacy is observed with 80% TGI and 20% of treated tumors indicating at least a 50% reduction in tumor volume. Oral administration of ABT-263 alone causes complete tumor regressions in xenograft models of small-cell lung cancer and acute lymphoblastic leukemia. In xenograft models of aggressive B-cell lymphoma and multiple myeloma where ABT-263 displays modest or no single agent activity, it significantly enhances the efficacy of clinically relevant therapeutic regimens.
Safety information: 
Additional information: 
Synonyms: HY-10087; ABT-263; ABT 263; ABT263
Hu L, Chen M, Chen X, et al. Chemotherapy-induced pyroptosis is mediated by BAK/BAX-caspase-3-GSDME pathway and inhibited by 2-bromopalmitate. Cell Death Dis. 2020;11(4):281. Read more
Bhola PD, Ahmed E, Guerriero JL, et al. High-throughput dynamic BH3 profiling may quickly and accurately predict effective therapies in solid tumors. Sci Signal. 2020;13(636) Read more
Wakita M, Takahashi A, Sano O, et al. A BET family protein degrader provokes senolysis by targeting NHEJ and autophagy in senescent cells. Nat Commun. 2020;11(1):1935. Read more
Mukherjee N, Skees J, Todd KJ, et al. MCL1 inhibitors S63845/MIK665 plus Navitoclax synergistically kill difficult-to-treat melanoma cells. Cell Death Dis. 2020;11(6):443. Read more
Haikala HM, Anttila JM, Marques E, et al. Pharmacological reactivation of MYC-dependent apoptosis induces susceptibility to anti-PD-1 immunotherapy. Nat Commun. 2019;10(1):620. Read more
Kauko O, O'connor CM, Kulesskiy E, et al. PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. Sci Transl Med. 2018;10(450) Read more