Original: 1NM-PP1 221244-14-0 , stock more than 100g

EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.

EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.

2018 CHINA CPHI, W4E82

EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com  
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.

Description: 1NM-PP1 is a potent Mutant Kinases Inhibitor.

Name: 1NM-PP1 

CAS#: 221244-14-0 

Chemical Formula: C20H21N5 

Exact Mass: 331.1797 

Molecular Weight: 331.41424 

Elemental Analysis: C, 72.48; H, 6.39; N, 21.13

Synonym: 1NM-PP1; 1NM PP1; 1NMPP1l PP1 analog II.

IUPAC/Chemical Name: 1-(tert-butyl)-3-(naphthalen-1-ylmethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

InChi Key: GDQXJQSQYMMKRA-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H21N5/c1-20(2,3)25-19-17(18(21)22-12-23-19)16(24-25)11-14-9-6-8-13-7-4-5-10-15(13)14/h4-10,12H,11H2,1-3H3,(H2,21,22,23)

SMILES Code: NC1=C2C(N(C(C)(C)C)N=C2CC3=C4C=CC=CC4=CC=C3)=NC=N1

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).

Harmonized System Code: 293490

ADDITIONAL INFORMATION

   

  

  

REFERENCES

1: Cadou A, Couturier A, Le Goff C, Xie L, Paulson JR, Le Goff X. The Kin1 kinase and the calcineurin phosphatase cooperate to link actin ring assembly and septum synthesis in fission yeast. Biol Cell. 2013 Mar;105(3):129-48. doi: 10.1111/boc.201200042. Epub 2013 Feb 8. PubMed PMID: 23294323.

2: Liang H, Lim HH, Venkitaraman A, Surana U. Cdk1 promotes kinetochore bi-orientation and regulates Cdc20 expression during recovery from spindle checkpoint arrest. EMBO J. 2012 Jan 18;31(2):403-16. doi: 10.1038/emboj.2011.385. Epub 2011 Nov 4. PubMed PMID: 22056777; PubMed Central PMCID: PMC3261552.

3: Sugi T, Kato K, Kobayashi K, Kurokawa H, Takemae H, Gong H, Recuenco FC, Iwanaga T, Horimoto T, Akashi H. 1NM-PP1 treatment of mice infected with Toxoplasma gondii. J Vet Med Sci. 2011 Oct;73(10):1377-9. Epub 2011 Jun 16. PubMed PMID: 21685719.

4: Haan C, Rolvering C, Raulf F, Kapp M, Drückes P, Thoma G, Behrmann I, Zerwes HG. Jak1 has a dominant role over Jak3 in signal transduction through γc-containing cytokine receptors. Chem Biol. 2011 Mar 25;18(3):314-23. doi: 10.1016/j.chembiol.2011.01.012. PubMed PMID: 21439476.

5: Sugi T, Kato K, Kobayashi K, Watanabe S, Kurokawa H, Gong H, Pandey K, Takemae H, Akashi H. Use of the kinase inhibitor analog 1NM-PP1 reveals a role for Toxoplasma gondii CDPK1 in the invasion step. Eukaryot Cell. 2010 Apr;9(4):667-70. doi: 10.1128/EC.00351-09. Epub 2010 Feb 19. PubMed PMID: 20173034; PubMed Central PMCID: PMC2863409.

6: Zuin A, Carmona M, Morales-Ivorra I, Gabrielli N, Vivancos AP, Ayté J, Hidalgo E. Lifespan extension by calorie restriction relies on the Sty1 MAP kinase stress pathway. EMBO J. 2010 Mar 3;29(5):981-91. doi: 10.1038/emboj.2009.407. Epub 2010 Jan 14. PubMed PMID: 20075862; PubMed Central PMCID: PMC2837171.

7: Wang X, Ratnam J, Zou B, England PM, Basbaum AI. TrkB signaling is required for both the induction and maintenance of tissue and nerve injury-induced persistent pain. J Neurosci. 2009 Apr 29;29(17):5508-15. doi: 10.1523/JNEUROSCI.4288-08.2009. PubMed PMID: 19403818; PubMed Central PMCID: PMC2720992.

8: Morgan DJ, Weisenhaus M, Shum S, Su T, Zheng R, Zhang C, Shokat KM, Hille B, Babcock DF, McKnight GS. Tissue-specific PKA inhibition using a chemical genetic approach and its application to studies on sperm capacitation. Proc Natl Acad Sci U S A. 2008 Dec 30;105(52):20740-5. doi: 10.1073/pnas.0810971105. Epub 2008 Dec 12. PubMed PMID: 19074277; PubMed Central PMCID: PMC2634883.

9: Wang H, Feng R, Phillip Wang L, Li F, Cao X, Tsien JZ. CaMKII activation state underlies synaptic labile phase of LTP and short-term memory formation. Curr Biol. 2008 Oct 28;18(20):1546-54. doi: 10.1016/j.cub.2008.08.064. Epub 2008 Oct 16. PubMed PMID: 18929487; PubMed Central PMCID: PMC2628633.

10: Kim JS, Lilley BN, Zhang C, Shokat KM, Sanes JR, Zhen M. A chemical-genetic strategy reveals distinct temporal requirements for SAD-1 kinase in neuronal polarization and synapse formation. Neural Dev. 2008 Sep 22;3:23. doi: 10.1186/1749-8104-3-23. PubMed PMID: 18808695; PubMed Central PMCID: PMC2564922.

Original: MDK-6149 508186-14-9 , stock more than 100g

EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.

EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.

2018 CHINA CPHI, W4E82

EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com  
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.

Description: MDK-6149, also known as ACSS2 Inhibitor or Ac-CoA Synthase Inhibitor I, is a Ac-CoA Synthase Inhibitor. MDK-6149 has CAS#508186-14-9. It was first reported in 2014. Cell. 159, 1591. For the convenience of scientific communication, we temporally name it as MDK-6149. The last 4 digit of its CAS# was used for name.

Name: MDK-6149 

CAS#: 508186-14-9 

Chemical Formula: C20H18N4O2S2 

Exact Mass: 410.0871 

Molecular Weight: 410.51 

Elemental Analysis: C, 58.52; H, 4.42; N, 13.65; O, 7.79; S, 15.62

Synonym: Ac-CoA Synthase Inhibitor I; MDK-6149; MDK 6149; MDK6149; ACSS2 Inhibitor

IUPAC/Chemical Name: 1-(2,3-di(Thiophen-2-yl)quinoxalin-6-yl)-3-(2-methoxyethyl)urea

InChi Key: CTPVNWVUAGMHEJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H18N4O2S2/c1-26-9-8-21-20(25)22-13-6-7-14-15(12-13)24-19(17-5-3-11-28-17)18(23-14)16-4-2-10-27-16/h2-7,10-12H,8-9H2,1H3,(H2,21,22,25)

SMILES Code: O=C(NCCOC)NC1=CC=C2N=C(C3=CC=CS3)C(C4=CC=CS4)=NC2=C1

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

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).

Harmonized System Code: 293490

REFERENCES

Comerford, S.A., et al. 2014. Cell. 159, 1591.

Original:BGB324 1037624-75-1 , stock more than 100g

EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.

EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.

2018 CHINA CPHI, W4E82

EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com  
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.

Description: BGB-324, also known as R428 or Bemcentinib, is a selective small molecule inhibitor of Axl kinase, which showed activity to blocks tumor spread and prolongs survival in models of metastatic breast cancer. The receptor tyrosine kinase Axl may play an important role in cancer progression, invasion, metastasis, drug resistance, and patient mortality. R428 inhibits Axl with low nanomolar activity and blocked Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production.

Name: BGB324 (R428) 
CAS#: 1037624-75-1 
Chemical Formula: C30H34N8 
Exact Mass: 506.29064 
Molecular Weight: 506.64 
Elemental Analysis: C, 71.12; H, 6.76; N, 22.12

Synonym: BGB324; BGB-324; BGB 324; R 428; R-428; R428; Bemcentinib;
IUPAC/Chemical Name: (S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine
InChi Key: KXMZDGSRSGHMMK-VWLOTQADSA-N
InChi Code: InChI=1S/C30H34N8/c31-29-33-30(32-24-13-10-20-11-14-25(15-12-22(20)18-24)37-16-3-4-17-37)36-38(29)27-19-23-8-5-7-21-6-1-2-9-26(21)28(23)35-34-27/h1-2,6,9-10,13,18-19,25H,3-5,7-8,11-12,14-17H2,(H3,31,32,33,36)/t25-/m0/s1

SMILES Code: NC1=NC(NC2=CC=C3C(CC[C@@H](N4CCCC4)CC3)=C2)=NN1C5=NN=C6C(CCCC7=CC=CC=C76)=C5

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).

Harmonized System Code: 293490

ADDITIONAL INFORMATION

   

  

  

REFERENCES

1: Hector A, Montgomery EA, Karikari C, Canto M, Dunbar KB, Wang JS, Feldmann G, Hong SM, Haffner MC, Meeker AK, Holland SJ, Yu J, Heckrodt TJ, Zhang J, Ding P, Goff D, Singh R, Roa JC, Marimuthu A, Riggins GJ, Eshleman JR, Nelkin BD, Pandey A, Maitra A. The Axl receptor tyrosine kinase is an adverse prognostic factor and a therapeutic target in esophageal adenocarcinoma. Cancer Biol Ther. 2010 Nov;10(10):1009-18. Epub 2010 Nov 15. PubMed PMID: 20818175; PubMed Central PMCID: PMC3025816.

2: Smolock EM, Korshunov VA. Pharmacological inhibition of Axl affects smooth muscle cell functions under oxidative stress. Vascul Pharmacol. 2010 Sep-Oct;53(3-4):185-92. Epub 2010 Jul 16. PubMed PMID: 20643227.

3: Holland SJ, Pan A, Franci C, Hu Y, Chang B, Li W, Duan M, Torneros A, Yu J, Heckrodt TJ, Zhang J, Ding P, Apatira A, Chua J, Brandt R, Pine P, Goff D, Singh R, Payan DG, Hitoshi Y. R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolongs survival in models of metastatic breast cancer. Cancer Res. 2010 Feb 15;70(4):1544-54. Epub 2010 Feb 9. PubMed PMID: 20145120.

Original: Idasanutlin 1229705-06-9 , stock more than 100g

EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.

EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.

2018 CHINA CPHI, W4E82

EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com  
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.

Description: Idasanutlin, also known as RG7388 and RO5503781, is a highly potent and selective MDM2 antagonist with potential anticancer activity. RG7388 binds to MDM2 blocking the interaction between the MDM2 protein and the transcriptional activation domain of the tumor suppressor protein p53. By preventing the MDM2-p53 interaction, p53 is not enzymatically degraded and the transcriptional activity of p53 is restored. This may lead to p53-mediated induction of tumor cell apoptosis. MDM2, a zinc finger nuclear phosphoprotein and negative regulator of the p53 pathway, is often overexpressed in cancer cells and has been implicated in cancer cell proliferation and survival.

Name: Idasanutlin (RG7388) 

CAS#: 1229705-06-9 

Chemical Formula: C31H29Cl2F2N3O4 

Exact Mass: 615.15032 

Molecular Weight: 616.48247 

Elemental Analysis: C, 60.40; H, 4.74; Cl, 11.50; F, 6.16; N, 6.82; O, 10.38

Synonym: RG7388; RG 7388; RG-7388; RO5503781; RO-5503781; RO 5503781; Idasanutlin.

IUPAC/Chemical Name: 4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoic acid.

InChi Key: TVTXCJFHQKSQQM-LJQIRTBHSA-N

InChi Code: InChI=1S/C31H29Cl2F2N3O4/c1-30(2,3)14-24-31(15-36,19-10-9-17(32)13-21(19)34)25(18-6-5-7-20(33)26(18)35)27(38-24)28(39)37-22-11-8-16(29(40)41)12-23(22)42-4/h5-13,24-25,27,38H,14H2,1-4H3,(H,37,39)(H,40,41)/t24-,25-,27+,31-/m0/s1

SMILES Code: O=C(O)C1=CC=C(NC([C@@H]2N[C@@H](CC(C)(C)C)[C@](C#N)(C3=CC=C(Cl)C=C3F)[C@H]2C4=CC=CC(Cl)=C4F)=O)C(OC)=C1

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).

Harmonized System Code: 293490

ADDITIONAL INFORMATION

   

REFERENCES

1: Ding Q, Zhang Z, Liu JJ, Jiang N, Zhang J, Ross TM, Chu XJ, Bartkovitz D, Podlaski F, Janson C, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev LT, Graves B. Discovery of RG7388, a Potent and Selective p53-MDM2 Inhibitor in Clinical Development. J Med Chem. 2013, 56 (14), 5979–5983.

Original: Verubecestat free base 1286770-55-5 , stock more than 100g

EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.

EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.

2018 CHINA CPHI, W4E82

EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com  
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.

Description: Verubecestat, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients.

Name: Verubecestat free base 

CAS#: 1286770-55-5 (free base) 

Chemical Formula: C17H17F2N5O3S 

Exact Mass: 409.102 

Molecular Weight: 409.41 

Elemental Analysis: C, 49.87; H, 4.19; F, 9.28; N, 17.11; O, 11.72; S, 7.83

Related CAS #: 2095432-65-6 (TFA)   1286770-55-5 (free base)   1875153-95-9 (Tosylate)   1970144-54-7 (HBr)   1897370-45-4 (hydrate)  

Synonym: MK-8931; MK 8931; MK8931; MK-8931-009; SCH 900931; SCH-900931; SCH900931; Verubecestat free base,

IUPAC/Chemical Name: (R)-N-(3-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2H-1,2,4-thiadiazin-5-yl)-4-fluorophenyl)-5-fluoropicolinamide

InChi Key: YHYKUSGACIYRML-KRWDZBQOSA-N

InChi Code: InChI=1S/C17H17F2N5O3S/c1-17(9-28(26,27)24(2)16(20)23-17)12-7-11(4-5-13(12)19)22-15(25)14-6-3-10(18)8-21-14/h3-8H,9H2,1-2H3,(H2,20,23)(H,22,25)/t17-/m0/s1

SMILES Code: O=C(NC1=CC=C(F)C([C@@](C2)(C)N=C(N)N(C)S2(=O)=O)=C1)C3=NC=C(F)C=C3

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

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).

Harmonized System Code: 293490

REFERENCES

1: Thaisrivongs DA, Morris WJ, Tan L, Song ZJ, Lyons TW, Waldman JH, Naber JR, Chen W, Chen L, Zhang B, Yang J. A Next Generation Synthesis of BACE1 Inhibitor Verubecestat (MK-8931). Org Lett. 2018 Mar 16;20(6):1568-1571. doi: 10.1021/acs.orglett.8b00259. Epub 2018 Feb 26. PubMed PMID: 29481097.

2: Chen W, Meng D, N'Zemba B, Morris WJ. Palladium-Catalyzed Enantioselective Synthesis of Cyclic Sulfamidates and Application to a Synthesis of Verubecestat. Org Lett. 2018 Mar 2;20(5):1265-1268. doi: 10.1021/acs.orglett.7b03639. Epub 2018 Feb 20. PubMed PMID: 29461065.

3: Barhate CL, Lopez DA, Makarov AA, Bu X, Morris WJ, Lekhal A, Hartman R, Armstrong DW, Regalado EL. Macrocyclic glycopeptide chiral selectors bonded to core-shell particles enables enantiopurity analysis of the entire verubecestat synthetic route. J Chromatogr A. 2018 Mar 2;1539:87-92. doi: 10.1016/j.chroma.2018.01.042. Epub 2018 Jan 31. PubMed PMID: 29397980.

4: Geerts H, Spiros A, Roberts P. Impact of amyloid-beta changes on cognitive outcomes in Alzheimer's disease: analysis of clinical trials using a quantitative systems pharmacology model. Alzheimers Res Ther. 2018 Feb 2;10(1):14. doi: 10.1186/s13195-018-0343-5. PubMed PMID: 29394903; PubMed Central PMCID: PMC5797372.

5: Villarreal S, Zhao F, Hyde LA, Holder D, Forest T, Sondey M, Chen X, Sur C, Parker EM, Kennedy ME. Chronic Verubecestat Treatment Suppresses Amyloid Accumulation in Advanced Aged Tg2576-AβPPswe Mice Without Inducing Microhemorrhage. J Alzheimers Dis. 2017;59(4):1393-1413. doi: 10.3233/JAD-170056. PubMed PMID: 28800329; PubMed Central PMCID: PMC5611839.

6: Prati F, Bottegoni G, Bolognesi ML, Cavalli A. BACE-1 Inhibitors: From Recent Single-Target Molecules to Multitarget Compounds for Alzheimer's Disease. J Med Chem. 2018 Feb 8;61(3):619-637. doi: 10.1021/acs.jmedchem.7b00393. Epub 2017 Aug 8. PubMed PMID: 28749667.

7: Hung SY, Fu WM. Drug candidates in clinical trials for Alzheimer's disease. J Biomed Sci. 2017 Jul 19;24(1):47. doi: 10.1186/s12929-017-0355-7. Review. PubMed PMID: 28720101; PubMed Central PMCID: PMC5516350.

8: Mullard A. BACE inhibitor bust in Alzheimer trial. Nat Rev Drug Discov. 2017 Mar 1;16(3):155. doi: 10.1038/nrd.2017.43. PubMed PMID: 28248932.

9: Hawkes N. Merck ends trial of potential Alzheimer's drug verubecestat. BMJ. 2017 Feb 15;356:j845. doi: 10.1136/bmj.j845. PubMed PMID: 28202490.

10: Thaisrivongs DA, Miller SP, Molinaro C, Chen Q, Song ZJ, Tan L, Chen L, Chen W, Lekhal A, Pulicare SK, Xu Y. Synthesis of Verubecestat, a BACE1 Inhibitor for the Treatment of Alzheimer's Disease. Org Lett. 2016 Nov 18;18(22):5780-5783. Epub 2016 Nov 4. PubMed PMID: 27934506.

11: Scott JD, Li SW, Brunskill AP, Chen X, Cox K, Cumming JN, Forman M, Gilbert EJ, Hodgson RA, Hyde LA, Jiang Q, Iserloh U, Kazakevich I, Kuvelkar R, Mei H, Meredith J, Misiaszek J, Orth P, Rossiter LM, Slater M, Stone J, Strickland CO, Voigt JH, Wang G, Wang H, Wu Y, Greenlee WJ, Parker EM, Kennedy ME, Stamford AW. Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer's Disease. J Med Chem. 2016 Dec 8;59(23):10435-10450. Epub 2016 Nov 18. PubMed PMID: 27933948.

12: Kennedy ME, Stamford AW, Chen X, Cox K, Cumming JN, Dockendorf MF, Egan M, Ereshefsky L, Hodgson RA, Hyde LA, Jhee S, Kleijn HJ, Kuvelkar R, Li W, Mattson BA, Mei H, Palcza J, Scott JD, Tanen M, Troyer MD, Tseng JL, Stone JA, Parker EM, Forman MS. The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients. Sci Transl Med. 2016 Nov 2;8(363):363ra150. PubMed PMID: 27807285.

13: Panza F, Seripa D, Solfrizzi V, Imbimbo BP, Lozupone M, Leo A, Sardone R, Gagliardi G, Lofano L, Creanza BC, Bisceglia P, Daniele A, Bellomo A, Greco A, Logroscino G. Emerging drugs to reduce abnormal β-amyloid protein in Alzheimer's disease patients. Expert Opin Emerg Drugs. 2016 Dec;21(4):377-391. Epub 2016 Oct 6. Review. PubMed PMID: 27678025.

14: Yan R. Stepping closer to treating Alzheimer's disease patients with BACE1 inhibitor drugs. Transl Neurodegener. 2016 Jul 14;5:13. doi: 10.1186/s40035-016-0061-5. eCollection 2016. Review. PubMed PMID: 27418961; PubMed Central PMCID: PMC4944430.

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