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2017年10月17日星期二

NMR, HPLC 99%, LCMS, Veliparib free base, CAS: 912444-00-9, 5G in stock, Pls check:

NMR, HPLC, LCMS, COA, Pls kindly check:




Description: Veliparib, also known as ABT-888, is a poly(ADP-ribose) polymerase (PARP) -1 and -2 inhibitor with chemosensitizing and antitumor activities. With no antiproliferative effects as a single agent at therapeutic concentrations, ABT-888 inhibits PARPs, thereby inhibiting DNA repair and potentiating the cytotoxicity of DNA-damaging agents.

Name: Veliparib free base 
CAS#: 912444-00-9 (free base) 
Chemical Formula: C13H16N4O 
Exact Mass: 244.13241 
Molecular Weight: 244.29 

Elemental Analysis: C, 63.91; H, 6.60; N, 22.93; O, 6.55

Related CAS #: 912444-00-9 (free base)   912445-05-7 (HCl)  
Synonym: ABT888; ABT-888; ABT 888; Veliparib
IUPAC/Chemical Name: (R)-2-(2-methylpyrrolidin-2-yl)-1H-benzo[d]imidazole-4-carboxamide
InChi Key: JNAHVYVRKWKWKQ-CYBMUJFWSA-N
InChi Code: InChI=1S/C13H16N4O/c1-13(6-3-7-15-13)12-16-9-5-2-4-8(11(14)18)10(9)17-12/h2,4-5,15H,3,6-7H2,1H3,(H2,14,18)(H,16,17)/t13-/m1/s1


TECHNICAL DATA
Appearance: White to off-white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Certificate of Analysis:  View CoA: previous batch, Lot#BBC60321 
 View CoA: previous batch, Lot#TZC70327 
 View CoA: current batch, Lot#T7K08C22 
QC Data:  View QC data: previous batch, Lot#BBC60321 
 View QC data: previous batch, Lot#TZC70327 
 View QC data: current batch, Lot#T7K08C22 
Safety Data Sheet (MSDS):  View Material Safety Data Sheet (MSDS) 
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

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REFERENCES
1: Bhute VJ, Ma Y, Bao X, Palecek SP. The Poly (ADP-Ribose) Polymerase Inhibitor Veliparib and Radiation Cause Significant Cell Line Dependent Metabolic Changes in Breast Cancer Cells. Sci Rep. 2016 Nov 4;6:36061. doi: 10.1038/srep36061. PubMed PMID: 27811964; PubMed Central PMCID: PMC5095763.
2: Ramalingam SS, Blais N, Mazieres J, Reck M, Jones CM, Juhász E, Urban L, Orlov S, Barlési F, Kio E, Keiholz U, Qin Q, Qian J, Nickner C, Dziubinski J, Xiong H, Ansell P, McKee MD, Giranda V, Gorbunova V. Randomized, Placebo-Controlled, Phase 2 Study of Veliparib in Combination with Carboplatin and Paclitaxel for Advanced/Metastatic Non-Small Cell Lung Cancer. Clin Cancer Res. 2016 Oct 10. pii: clincanres.3069.2016. [Epub ahead of print] PubMed PMID: 27803064.
3: Munasinghe W, Stodtmann S, Tolcher A, Calvo E, Gordon M, Jalving M, de Vos-Geelen J, Medina D, Bergau D, Nuthalapati S, Hoffman D, Shepherd S, Xiong H. Effect of veliparib (ABT-888) on cardiac repolarization in patients with advanced solid tumors: a randomized, placebo-controlled crossover study. Cancer Chemother Pharmacol. 2016 Nov;78(5):1003-1011. PubMed PMID: 27709282; PubMed Central PMCID: PMC5083757.
4: Isakoff SJ, Puhalla S, Domchek SM, Friedlander M, Kaufman B, Robson M, Telli ML, Diéras V, Han HS, Garber JE, Johnson EF, Maag D, Qin Q, Giranda VL, Shepherd SP. A randomized Phase II study of veliparib with temozolomide or carboplatin/paclitaxel versus placebo with carboplatin/paclitaxel in BRCA1/2 metastatic breast cancer: design and rationale. Future Oncol. 2016 Oct 14. [Epub ahead of print] PubMed PMID: 27739325.
5: Chabot P, Hsia TC, Ryu JS, Gorbunova V, Belda-Iniesta C, Ball D, Kio E, Mehta M, Papp K, Qin Q, Qian J, Holen KD, Giranda V, Suh JH. Veliparib in combination with whole-brain radiation therapy for patients with brain metastases from non-small cell lung cancer: results of a randomized, global, placebo-controlled study. J Neurooncol. 2016 Sep 21. [Epub ahead of print] PubMed PMID: 27655223.
6: Subhash VV, Tan SH, Yeo MS, Yan FL, Peethala PC, Liem N, Krishnan V, Yong WP. ATM expression predicts Veliparib and Irinotecan sensitivity in gastric cancer by mediating P53 independent regulation of cell cycle and apoptosis. Mol Cancer Ther. 2016 Sep 16. pii: molcanther.1002.2015. [Epub ahead of print] PubMed PMID: 27638859.
7: Pratz KW, Rudek MA, Gojo I, Litzow MR, McDevitt MA, Ji JJ, Karnitz L, Herman JG, Kinders R, Smith BD, Gore SD, Carraway H, Showel MM, Gladstone DE, Levis MJ, Tsai HL, Rosner GL, Chen A, Kaufmann SH, Karp J. A Phase I study of topotecan, carboplatin and the PARP inhibitor veliparib in acute leukemias, aggressive myeloproliferative neoplasms and chronic myelomonocytic leukemia. Clin Cancer Res. 2016 Aug 22. pii: clincanres.1274.2016. [Epub ahead of print] PubMed PMID: 27551000.
8: Gojo I, Beumer JH, Pratz KW, McDevitt MA, Baer MR, Blackford AL, Smith BD, Gore SD, Carraway H, Showel MM, Levis MJ, Dezern A, Gladstone DE, Ji JJ, Wang L, Kinders R, Pouquet M, Ali-Walbi I, Rudek MA, Poh W, Herman JG, Karnitz L, Kaufmann SH, Chen A, Karp J. A phase 1 study of the PARP inhibitor veliparib in combination with temozolomide in acute myeloid leukemia. Clin Cancer Res. 2016 Aug 8. pii: clincanres.0984.2016. [Epub ahead of print] PubMed PMID: 27503200.
9: Rugo HS, Olopade OI, DeMichele A, Yau C, van 't Veer LJ, Buxton MB, Hogarth M, Hylton NM, Paoloni M, Perlmutter J, Symmans WF, Yee D, Chien AJ, Wallace AM, Kaplan HG, Boughey JC, Haddad TC, Albain KS, Liu MC, Isaacs C, Khan QJ, Lang JE, Viscusi RK, Pusztai L, Moulder SL, Chui SY, Kemmer KA, Elias AD, Edmiston KK, Euhus DM, Haley BB, Nanda R, Northfelt DW, Tripathy D, Wood WC, Ewing C, Schwab R, Lyandres J, Davis SE, Hirst GL, Sanil A, Berry DA, Esserman LJ; I-SPY 2 Investigators.. Adaptive Randomization of Veliparib-Carboplatin Treatment in Breast Cancer. N Engl J Med. 2016 Jul 7;375(1):23-34. doi: 10.1056/NEJMoa1513749. PubMed PMID: 27406347.
10: Kummar S, Wade JL, Oza AM, Sullivan D, Chen AP, Gandara DR, Ji J, Kinders RJ, Wang L, Allen D, Coyne GO, Steinberg SM, Doroshow JH. Randomized phase II trial of cyclophosphamide and the oral poly (ADP-ribose) polymerase inhibitor veliparib in patients with recurrent, advanced triple-negative breast cancer. Invest New Drugs. 2016 Jun;34(3):355-63. doi: 10.1007/s10637-016-0335-x. PubMed PMID: 26996385; PubMed Central PMCID: PMC4860030.
11: Villalona-Calero MA, Duan W, Zhao W, Shilo K, Schaaf LJ, Thurmond J, Westman JA, Marshall J, Xiaobai L, Ji J, Rose J, Lustberg M, Bekaii-Saab T, Chen A, Timmers C. Veliparib Alone or in Combination with Mitomycin C in Patients with Solid Tumors With Functional Deficiency in Homologous Recombination Repair. J Natl Cancer Inst. 2016 Feb 4;108(7). pii: djv437. doi: 10.1093/jnci/djv437. PubMed PMID: 26848151; PubMed Central PMCID: PMC4948564.
12: LoRusso PM, Li J, Burger A, Heilbrun LK, Sausville EA, Boerner SA, Smith D, Pilat MJ, Zhang J, Tolaney SM, Cleary JM, Chen AP, Rubinstein L, Boerner JL, Bowditch A, Cai D, Bell T, Wolanski A, Marrero AM, Zhang Y, Ji J, Ferry-Galow K, Kinders RJ, Parchment RE, Shapiro GI. Phase I Safety, Pharmacokinetic, and Pharmacodynamic Study of the Poly(ADP-ribose) Polymerase (PARP) Inhibitor Veliparib (ABT-888) in Combination with Irinotecan in Patients with Advanced Solid Tumors. Clin Cancer Res. 2016 Jul 1;22(13):3227-37. doi: 10.1158/1078-0432.CCR-15-0652. PubMed PMID: 26842236; PubMed Central PMCID: PMC4930710.
13: Bogliolo S, Cassani C, Dominoni M, Musacchi V, Venturini PL, Spinillo A, Ferrero S, Gardella B. Veliparib for the treatment of ovarian cancer. Expert Opin Investig Drugs. 2016;25(3):367-74. doi: 10.1517/13543784.2016.1146677. Review. PubMed PMID: 26807493.
14: Rodler ET, Kurland BF, Griffin M, Gralow JR, Porter P, Yeh RF, Gadi VK, Guenthoer J, Beumer JH, Korde L, Strychor S, Kiesel BF, Linden HM, Thompson JA, Swisher E, Chai X, Shepherd S, Giranda V, Specht JM. Phase I Study of Veliparib (ABT-888) Combined with Cisplatin and Vinorelbine in Advanced Triple-Negative Breast Cancer and/or BRCA Mutation-Associated Breast Cancer. Clin Cancer Res. 2016 Jun 15;22(12):2855-64. doi: 10.1158/1078-0432.CCR-15-2137. PubMed PMID: 26801247; PubMed Central PMCID: PMC4911292.
15: Landrum LM, Brady WE, Armstrong DK, Moore KN, DiSilvestro PA, O'Malley DM, Tenney ME, Rose PG, Fracasso PM. A phase I trial of pegylated liposomal doxorubicin (PLD), carboplatin, bevacizumab and veliparib in recurrent, platinum-sensitive ovarian, primary peritoneal, and fallopian tube cancer: An NRG Oncology/Gynecologic Oncology Group study. Gynecol Oncol. 2016 Feb;140(2):204-9. doi: 10.1016/j.ygyno.2015.11.024. PubMed PMID: 26616225; PubMed Central PMCID: PMC4724478.
16: Gupta SK, Kizilbash SH, Carlson BL, Mladek AC, Boakye-Agyeman F, Bakken KK, Pokorny JL, Schroeder MA, Decker PA, Cen L, Eckel-Passow JE, Sarkar G, Ballman KV, Reid JM, Jenkins RB, Verhaak RG, Sulman EP, Kitange GJ, Sarkaria JN. Delineation of MGMT Hypermethylation as a Biomarker for Veliparib-Mediated Temozolomide-Sensitizing Therapy of Glioblastoma. J Natl Cancer Inst. 2015 Nov 27;108(5). pii: djv369. doi: 10.1093/jnci/djv369. PubMed PMID: 26615020; PubMed Central PMCID: PMC4862419.
17: Gabrielson A, Tesfaye AA, Marshall JL, Pishvaian MJ, Smaglo B, Jha R, Dorsch-Vogel K, Wang H, He AR. Phase II study of temozolomide and veliparib combination therapy for sorafenib-refractory advanced hepatocellular carcinoma. Cancer Chemother Pharmacol. 2015 Nov;76(5):1073-9. doi: 10.1007/s00280-015-2852-2. PubMed PMID: 26449224; PubMed Central PMCID: PMC4612326.
18: Mizugaki H, Yamamoto N, Nokihara H, Fujiwara Y, Horinouchi H, Kanda S, Kitazono S, Yagishita S, Xiong H, Qian J, Hashiba H, Shepherd SP, Giranda V, Tamura T. A phase 1 study evaluating the pharmacokinetics and preliminary efficacy of veliparib (ABT-888) in combination with carboplatin/paclitaxel in Japanese subjects with non-small cell lung cancer (NSCLC). Cancer Chemother Pharmacol. 2015 Nov;76(5):1063-72. doi: 10.1007/s00280-015-2876-7. PubMed PMID: 26433581; PubMed Central PMCID: PMC4612330.
19: VanderWeele DJ, Paner GP, Fleming GF, Szmulewitz RZ. Sustained Complete Response to Cytotoxic Therapy and the PARP Inhibitor Veliparib in Metastatic Castration-Resistant Prostate Cancer - A Case Report. Front Oncol. 2015 Jul 22;5:169. doi: 10.3389/fonc.2015.00169. PubMed PMID: 26258074; PubMed Central PMCID: PMC4510409.