Veliparib

  • CAT Number: I005438
  • CAS Number: 912444-00-9
  • Molecular Formula: C13H16N4O
  • Molecular Weight: 244.3
  • Purity: ≥95%
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Veliparib (CAT: I005438) is a pharmaceutical compound belonging to the class of poly(ADP-ribose) polymerase (PARP) inhibitors. It functions by inhibiting the activity of PARP enzymes, which are involved in DNA repair processes. By blocking PARP, veliparib prevents cancer cells from repairing DNA damage, leading to their accumulation and eventual death. Veliparib has been investigated for its potential in cancer treatment, particularly in combination with chemotherapy or radiation therapy. It is being studied in various types of cancer, including ovarian, breast, lung, and prostate cancer. Clinical trials aim to evaluate its effectiveness and safety as a targeted therapy for these malignancies.

Catalog Number I005438
CAS Number 912444-00-9
Molecular Formula

C13H16N4O

Purity 95%
Target PARP
Solubility DMSO: ≥ 29 mg/mL
Storage <label class=
IC50 5.2 nM(Ki for PARP1); 2.9 nM(Ki for PARP2)
IUPAC Name 2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide
InChI 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
InChIKey JNAHVYVRKWKWKQ-CYBMUJFWSA-N
SMILES O=C(C1=C2C(NC([C@]3(C)NCCC3)=N2)=CC=C1)N
Reference

1: Czito BG, Deming DA, Jameson GS, Mulcahy MF, Vaghefi H, Dudley MW, Holen KD, DeLuca A, Mittapalli RK, Munasinghe W, He L, Zalcberg JR, Ngan SY, Komarnitsky P, Michael M. Safety and tolerability of veliparib combined with capecitabine plus radiotherapy in patients with locally advanced rectal cancer: a phase 1b study. Lancet Gastroenterol Hepatol. 2017 Jun;2(6):418-426. doi: 10.1016/S2468-1253(17)30012-2. Epub 2017 Mar 27. PubMed PMID: 28497757.<br />
2: Nuthalapati S, Munasinghe W, Giranda V, Xiong H. Clinical Pharmacokinetics and Mass Balance of Veliparib in Combination with Temozolomide in Subjects with Nonhematologic Malignancies. Clin Pharmacokinet. 2017 May 11. doi: 10.1007/s40262-017-0547-z. [Epub ahead of print] PubMed PMID: 28497258.<br />
3: Mittapalli RK, Nuthalapati S, Delke DeBord AE, Xiong H. Development of a Level A in Vitro-in Vivo Correlation for Veliparib (ABT-888) Extended Release Tablet Formulation. Pharm Res. 2017 Jun;34(6):1187-1192. doi: 10.1007/s11095-017-2133-3. Epub 2017 Feb 27. PubMed PMID: 28243955.<br />
4: Reck M, Blais N, Juhasz E, Gorbunova V, Jones CM, Urban L, Orlov S, Barlesi F, Kio E, Keilholz U, Qin Q, Qian J, Nickner C, Dziubinski J, Xiong H, Mittapalli RK, Dunbar M, Ansell P, He L, McKee M, Giranda V, Ramalingam SS. Smoking History Predicts Sensitivity to PARP Inhibitor Veliparib in Patients with Advanced Non-Small Cell Lung Cancer. J Thorac Oncol. 2017 Apr 29. pii: S1556-0864(17)30338-6. doi: 10.1016/j.jtho.2017.04.010. [Epub ahead of print] PubMed PMID: 28461256.<br />
5: Soumerai JD, Zelenetz AD, Moskowitz CH, Palomba ML, Hamlin PA Jr, Noy A, Straus DJ, Moskowitz AJ, Younes A, Matasar MJ, Horwitz SM, Portlock CS, Konner JA, Gounder MM, Hyman DM, Voss MH, Fury MG, Gajria D, Carvajal RD, Ho AL, Beumer JH, Kiesel B, Zhang Z, Chen A, Little RF, Jarjies C, Dang TO, France F, Mishra N, Gerecitano JF. The PARP Inhibitor Veliparib Can Be Safely Added to Bendamustine and Rituximab and Has Preliminary Evidence of Activity in B-Cell Lymphoma. Clin Cancer Res. 2017 Mar 17. doi: 10.1158/1078-0432.CCR-16-3068. [Epub ahead of print] PubMed PMID: 28314788.<br />
6: Jue TR, Nozue K, Lester AJ, Joshi S, Schroder LB, Whittaker SP, Nixdorf S, Rapkins RW, Khasraw M, McDonald KL. Veliparib in combination with radiotherapy for the treatment of MGMT unmethylated glioblastoma. J Transl Med. 2017 Mar 17;15(1):61. doi: 10.1186/s12967-017-1164-1. PubMed PMID: 28314386; PubMed Central PMCID: PMC5356284.<br />
7: Reiss KA, Herman JM, Armstrong D, Zahurak M, Fyles A, Brade A, Milosevic M, Dawson LA, Scardina A, Fischer P, Hacker-Prietz A, Kinders RJ, Wang L, Chen A, Temkin S, Horiba N, Stayner LA, Siu LL, Azad NS. A final report of a phase I study of veliparib (ABT-888) in combination with low-dose fractionated whole abdominal radiation therapy (LDFWAR) in patients with advanced solid malignancies and peritoneal carcinomatosis with a dose escalation in ovarian and fallopian tube cancers. Gynecol Oncol. 2017 Mar;144(3):486-490. doi: 10.1016/j.ygyno.2017.01.016. Epub 2017 Jan 18. PubMed PMID: 28109627; PubMed Central PMCID: PMC5330287.<br />
8: Mehrotra S, Gopalakrishnan M, Gobburu J, Greer JM, Piekarz R, Karp JE, Pratz K, Rudek MA. Population pharmacokinetics and site of action exposures of veliparib with topotecan plus carboplatin in patients with haematological malignancies. Br J Clin Pharmacol. 2017 Feb 3. doi: 10.1111/bcp.13253. [Epub ahead of print] PubMed PMID: 28156017.<br />
9: 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. 2017 Jan;131(1):105-115. doi: 10.1007/s11060-016-2275-x. Epub 2016 Sep 21. PubMed PMID: 27655223; PubMed Central PMCID: PMC5258788.<br />
10: Niu J, Scheuerell C, Mehrotra S, Karan S, Puhalla S, Kiesel BF, Ji J, Chu E, Gopalakrishnan M, Ivaturi V, Gobburu J, Beumer JH. Parent-Metabolite Pharmacokinetic Modeling and Pharmacodynamics of Veliparib (ABT-888), a PARP Inhibitor, in Patients With BRCA 1/2-Mutated Cancer or PARP-Sensitive Tumor Types. J Clin Pharmacol. 2017 Apr 7. doi: 10.1002/jcph.892. [Epub ahead of print] PubMed PMID: 28387939.

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