Navitoclax

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WARNING: This product is for research use only, not for human or veterinary use.

Description:Navitoclax, also known as ABT-263, is an orally bioavailable, synthetic small-molecule antagonist of a subset of the B-cell leukemia 2 (Bcl-2) family of proteins with potential antineoplastic activity. ABT-263 selectively binds to apoptosis suppressor proteins Bcl-2, Bcl-XL, and Bcl-w and prevents their binding to the apoptotic effectors Bax and Bak proteins, which may trigger apoptosis in tumor cells overexpressing Bcl-2, Bcl-XL, and Bcl-w.

Price and Availability

Navitoclax, purity > 98%, is in stock. The same day shipping after order is received.

Synonym:ABT 263; ABT-263; ABT263; Navitoclax

IUPAC/Chemical Name:(R)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide

InChi Key:JLYAXFNOILIKPP-KXQOOQHDSA-N

InChi Code:InChI=1S/C47H55ClF3N5O6S3/c1-46(2)20-18-42(34-8-12-37(48)13-9-34)36(31-46)32-55-22-24-56(25-23-55)39-14-10-35(11-15-39)45(57)53-65(60,61)41-16-17-43(44(30-41)64(58,59)47(49,50)51)52-38(19-21-54-26-28-62-29-27-54)33-63-40-6-4-3-5-7-40/h3-17,30,38,52H,18-29,31-33H2,1-2H3,(H,53,57)/t38-/m1/s1

SMILES Code:O=C(NS(=O)(C1=CC=C(N[C@H](CCN2CCOCC2)CSC3=CC=CC=C3)C(S(=O)(C(F)(F)F)=O)=C1)=O)C4=CC=C(N5CCN(CC6=C(C7=CC=C(Cl)C=C7)CCC(C)(C)C6)CC5)C=C4

Technical Data

Additional Information

Bcl-2, Bcl-XL, and Bcl-w are frequently overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon, and have been linked to tumor drug resistance.

References

1: Kaefer A, Yang J, Noertersheuser P, Mensing S,Humerickhouse R, Awni W, Xiong H. Mechanism-based pharmacokinetic/pharmacodynamicmeta-analysis of navitoclax (ABT-263) induced thrombocytopenia. CancerChemother Pharmacol. 2014 Sep;74(3):593-602. doi:10.1007/s00280-014-2530-9. Epub 2014 Jul 23. PubMed PMID: 25053389.

2: Yang J, Pradhan RS, Rosen LS, Graham AM, Holen KD, Xiong H. Effect ofrifampin on the pharmacokinetics, safety and tolerability of navitoclax(ABT-263), a dual inhibitor of Bcl-2 and Bcl-X(L) , in patients withcancer. J Clin Pharm Ther. 2014 Jul 22. doi: 10.1111/jcpt.12193. [Epubahead of print] PubMed PMID: 25047139.

3: Wei X, Zhou P, Lin X, Lin Y, Wu S, Diao P, Xie H, Xie K, Tang P.MLN2238 synergizes BH3 mimetic ABT-263 in castration-resistant prostatecancer cells by induction of NOXA. Tumour Biol. 2014 Jul 17. [Epub aheadof print] PubMed PMID: 25027405.

4: Suryani S, Carol H, Chonghaile TN, Frismantas V, Sarmah C, High L,Bornhauser B, Cowley MJ, Szymanska B, Evans K, Boehm I, Tonna E, JonesL, Manesh DM, Kurmasheva RT, Billups C, Kaplan W, Letai A, Bourquin JP,Houghton PJ, Smith MA, Lock RB. Cell and Molecular Determinants of InVivo Efficacy of the BH3 Mimetic ABT-263 against Pediatric AcuteLymphoblastic Leukemia Xenografts. Clin Cancer Res. 2014 Sep1;20(17):4520-31. doi: 10.1158/1078-0432.CCR-14-0259. Epub 2014 Jul 10.PubMed PMID: 25013123; PubMed Central PMCID: PMC4154988.

5: Polier G, Giaisi M, Köhler R, Müller WW, Lutz C, Buss EC, Krammer PH,Li-Weber M. Targeting CDK9 by wogonin and related natural flavonespotentiates the anti-cancer efficacy of the Bcl-2 family inhibitorABT-263. Int J Cancer. 2014 Jun 4. doi: 10.1002/ijc.29009. [Epub aheadof print] PubMed PMID: 24895203.

6: Vlahovic G, Karantza V, Wang D, Cosgrove D, Rudersdorf N, Yang J,Xiong H, Busman T, Mabry M. A phase I safety and pharmacokinetic studyof ABT-263 in combination with carboplatin/paclitaxel in the treatmentof patients with solid tumors. Invest New Drugs. 2014 Oct;32(5):976-84.doi: 10.1007/s10637-014-0116-3. Epub 2014 Jun 5. PubMed PMID: 24894650.

7: Wang X, Gu Z, Li G, Zhang S, Cao Z, Yang Z, Liu G. Norcantharidinenhances ABT-263-mediated anticancer activity in neuroblastoma cells byupregulation of Noxa. Oncol Rep. 2014 Aug;32(2):716-22. doi:10.3892/or.2014.3228. Epub 2014 May 30. PubMed PMID: 24891300.

8: Wang B, Ni Z, Dai X, Qin L, Li X, Xu L, Lian J, He F. The Bcl-2/xLinhibitor ABT-263 increases the stability of Mcl-1 mRNA and protein inhepatocellular carcinoma cells. Mol Cancer. 2014 Apr 30;13:98. doi:10.1186/1476-4598-13-98. PubMed PMID: 24779770; PubMed Central PMCID:PMC4021276.

9: Li J, Chen Y, Wan J, Liu X, Yu C, Li W. ABT-263 enhances sorafenib-inducedapoptosis associated with Akt activity and the expression of Bax andp21((CIP1/WAF1)) in human cancer cells. Br J Pharmacol. 2014Jul;171(13):3182-95. doi: 10.1111/bph.12659. PubMed PMID: 24571452;PubMed Central PMCID: PMC4080973.

10: Choo EF, Boggs J, Zhu C, Lubach JW, Catron ND, Jenkins G, Souers AJ,Voorman R. The role of lymphatic transport on the systemicbioavailability of the Bcl-2 protein family inhibitors navitoclax(ABT-263) and ABT-199. Drug Metab Dispos. 2014 Feb;42(2):207-12. doi:10.1124/dmd.113.055053. Epub 2013 Nov 8. PubMed PMID: 24212376.

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