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Product name : CBL0137
Item : C2446
Price : 200mg, $950;500mg, $1695; 1g, $2490; 2g, $3590
contact : Send inquiry to: info@acesobio.com
CAS : 1197996-80-7
Molecular Weight : 336.435
Formula : C21H24N2O2
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order.
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Details:
Description of:CBL0137(CAS:1197996-80-7)
CBL0137, also known as Curaxin 137, is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM. CBL0137 inhibits histone chaperone FACT, is efficacious in preclinical orthotopic models of temozolomide-responsive and -resistant glioblastoma. CBL0137 eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer.

Quality control data:
Quality control by 1H-NMR, 13C-NMR, HPLC and LCMS.
Product will be shipped with supporting analytical data.

REFERENCES

1: Fleyshman D, Prendergast L, Safina A, Paszkiewicz G, Commane M, Morgan K, Attwood K, Gurova K. Level of FACT defines the transcriptional landscape and aggressive phenotype of breast cancer cells. Oncotarget. 2017 Mar 28;8(13):20525-20542. doi: 10.18632/oncotarget.15656. PubMed PMID: 28423528; PubMed Central PMCID: PMC5400524.

2: Kim M, Neznanov N, Wilfong CD, Fleyshman DI, Purmal AA, Haderski G, Stanhope-Baker P, Burkhart CA, Gurova KV, Gudkov AV, Skitzki JJ. Preclinical Validation of a Single-Treatment Infusion Modality That Can Eradicate Extremity Melanomas. Cancer Res. 2016 Nov 15;76(22):6620-6630. doi: 10.1158/0008-5472.CAN-15-2764. Epub 2016 Sep 28. PubMed PMID: 27680682; PubMed Central PMCID: PMC5609527.

3: Maluchenko NV, Chang HW, Kozinova MT, Valieva ME, Gerasimova NS, Kitashov AV, Kirpichnikov MP, Georgiev PG, Studitsky VM. [Inhibiting the pro-tumor and transcription factor FACT: Mechanisms]. Mol Biol (Mosk). 2016 Jul-Aug;50(4):599-610. Russian. PubMed PMID: 27668600.

4: Lock R, Carol H, Maris JM, Kolb EA, Gorlick R, Reynolds CP, Kang MH, Keir ST, Wu J, Purmal A, Gudkov A, Kurmashev D, Kurmasheva RT, Houghton PJ, Smith MA. Initial testing (stage 1) of the curaxin CBL0137 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2017 Apr;64(4). doi: 10.1002/pbc.26263. Epub 2016 Sep 21. PubMed PMID: 27650817; PubMed Central PMCID: PMC5587189.

5: Barone TA, Burkhart CA, Safina A, Haderski G, Gurova KV, Purmal AA, Gudkov AV, Plunkett RJ. Anticancer drug candidate CBL0137, which inhibits histone chaperone FACT, is efficacious in preclinical orthotopic models of temozolomide-responsive and -resistant glioblastoma. Neuro Oncol. 2017 Feb 1;19(2):186-196. doi: 10.1093/neuonc/now141. PubMed PMID: 27370399; PubMed Central PMCID: PMC5604960.

6: Dermawan JK, Hitomi M, Silver DJ, Wu Q, Sandlesh P, Sloan AE, Purmal AA, Gurova KV, Rich JN, Lathia JD, Stark GR, Venere M. Pharmacological Targeting of the Histone Chaperone Complex FACT Preferentially Eliminates Glioblastoma Stem Cells and Prolongs Survival in Preclinical Models. Cancer Res. 2016 Apr 15;76(8):2432-42. doi: 10.1158/0008-5472.CAN-15-2162. Epub 2016 Feb 26. PubMed PMID: 26921329; PubMed Central PMCID: PMC4873320.

7: Carter DR, Murray J, Cheung BB, Gamble L, Koach J, Tsang J, Sutton S, Kalla H, Syed S, Gifford AJ, Issaeva N, Biktasova A, Atmadibrata B, Sun Y, Sokolowski N, Ling D, Kim PY, Webber H, Clark A, Ruhle M, Liu B, Oberthuer A, Fischer M, Byrne J, Saletta F, Thwe le M, Purmal A, Haderski G, Burkhart C, Speleman F, De Preter K, Beckers A, Ziegler DS, Liu T, Gurova KV, Gudkov AV, Norris MD, Haber M, Marshall GM. Therapeutic targeting of the MYC signal by inhibition of histone chaperone FACT in neuroblastoma. Sci Transl Med. 2015 Nov 4;7(312):312ra176. doi: 10.1126/scitranslmed.aab1803. PubMed PMID: 26537256.

8: Burkhart C, Fleyshman D, Kohrn R, Commane M, Garrigan J, Kurbatov V, Toshkov I, Ramachandran R, Martello L, Gurova KV. Curaxin CBL0137 eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer. Oncotarget. 2014 Nov 30;5(22):11038-53. PubMed PMID: 25402820; PubMed Central PMCID: PMC4294371.

9: Gasparian AV, Burkhart CA, Purmal AA, Brodsky L, Pal M, Saranadasa M, Bosykh DA, Commane M, Guryanova OA, Pal S, Safina A, Sviridov S, Koman IE, Veith J, Komar AA, Gudkov AV, Gurova KV. Curaxins: anticancer compounds that simultaneously suppress NF-κB and activate p53 by targeting FACT. Sci Transl Med. 2011 Aug 10;3(95):95ra74. doi: 10.1126/scitranslmed.3002530. PubMed PMID: 21832239.



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