EOS Med Chem, Medicinal Chemical is Big

2018年5月6日星期日

Original:ML130 799264-47-4 , 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.

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2018 CHINA CPHI, W4E82

EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
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Description: ML130 is an inhibitor of NOD1 (nucleotide-binding oligomerization domain containing 1).

Name: ML130

CAS#: 799264-47-4

Chemical Formula: C14H13N3O2S

Exact Mass: 287.0728

Molecular Weight: 287.34

Elemental Analysis: C, 58.52; H, 4.56; N, 14.62; O, 11.14; S, 11.16

Synonym: ML130; ML 130; ML-130.

IUPAC/Chemical Name: 1-(4-methylphenyl)sulfonylbenzimidazol-2-amine

InChi Key: SRFABRWQVPCPRG-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H13N3O2S/c1-10-6-8-11(9-7-10)20(18,19)17-13-5-3-2-4-12(13)16-14(17)15/h2-9H,1H3,(H2,15,16)

SMILES Code: NC1=NC2=CC=CC=C2N1S(=O)(C3=CC=C(C)C=C3)=OInChI=1S/C14H13N3O2S/c1-10-6-8-11(9-7-10)20(18,19)17-13-5-3-2-4-12(13)16-14(17)15/h2-9H,1H3,(H2,15,16)

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: Fan YH, Roy S, Mukhopadhyay R, Kapoor A, Duggal P, Wojcik GL, Pass RF, Arav-Boger R. Role of nucleotide-binding oligomerization domain 1 (NOD1) and its variants in human cytomegalovirus control in vitro and in vivo. Proc Natl Acad Sci U S A. 2016 Nov 29;113(48):E7818-E7827. PubMed PMID: 27856764; PubMed Central PMCID: PMC5137695.

2: Wei LJ, Tan X, Fan GJ, Jiang YN, Shah QA. Role of the NOD1/NF-κB pathway on bovine neutrophil responses to crude lipopolysaccharide. Vet J. 2016 Aug;214:24-31. doi: 10.1016/j.tvjl.2016.02.006. PubMed PMID: 27387722.

Original: AA26-9 1312782-34-5 , stock more than 100g

2018 CHINA CPHI, W4E82

Description: AA26-9 is a potent and broad-spectrum serine hydrolase inhibitor. AA26-9-inhibited enzymes originated from diverse functional subclasses of serine hydrolases, including lipases/phospholipases, thioesterases, and uncharacterized enzymes.

Name: AA26-9

CAS#: 1312782-34-5

Chemical Formula: C7H10N4O

Exact Mass: 166.0855

Molecular Weight: 166.184

Elemental Analysis: C, 50.59; H, 6.07; N, 33.71; O, 9.63

Synonym: AA 26-9; AA-26-9; AA26-9; AA 269; AA-269; AA269;

IUPAC/Chemical Name: Pyrrolidin-1-yl(triazol-1-yl)methanone

InChi Key: IFXGAMVQLDJRBQ-UHFFFAOYSA-N

InChi Code: InChI=1S/C7H10N4O/c12-7(10-4-1-2-5-10)11-6-3-8-9-11/h3,6H,1-2,4-5H2

SMILES Code: O=C(N1CCCC1)N2N=NC=C2

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

Adibekian A, et al. Click-generated triazole ureas as ultrapotent in vivo-active serine hydrolase inhibitors. Nat Chem Biol. 2011 May 15;7(7):469-78.

Original:BQCA 338747-41-4 , stock more than 100g

2018 CHINA CPHI, W4E82

Description: BQCA is a potent muscarinic M1 receptor positive allosteric modulator with selectivity for M1 over M2-M5. Stimulation of the cortical muscarinic M1 receptor (CHRM1) is proposed as a treatment for schizophrenia, a hypothesis testable using CHRM1 allosteric modulators. BQCA binds allosterically to M1 to enhance the binding and efficacy of ACh at the receptor. M1 activation is a proposed mechanism for increasing information processing in disease states, such as Alzheimer′s.

Name: BQCA

CAS#: 338747-41-4

Chemical Formula: C18H15NO4

Exact Mass: 309.1001

Molecular Weight: 309.321

Elemental Analysis: C, 69.89; H, 4.89; N, 4.53; O, 20.69

Synonym: BQCA, CAS#338747-41-4.

IUPAC/Chemical Name: 1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

InChi Key: BZBBTGCKPRSPGF-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H15NO4/c1-23-13-8-6-12(7-9-13)10-19-11-15(18(21)22)17(20)14-4-2-3-5-16(14)19/h2-9,11H,10H2,1H3,(H,21,22)

SMILES Code: O=C(C1=CN(CC2=CC=C(OC)C=C2)C3=C(C=CC=C3)C1=O)O

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

REFERENCES

1: Dean B, Hopper S, Conn PJ, Scarr E. Changes in BQCA Allosteric Modulation of

[(3)H]NMS Binding to Human Cortex within Schizophrenia and by Divalent Cations.

Neuropsychopharmacology. 2015 Oct 29. doi: 10.1038/npp.2015.330. [Epub ahead of

print] PubMed PMID: 26511338.

2: Davie BJ, Valant C, White JM, Sexton PM, Capuano B, Christopoulos A, Scammells

PJ. Synthesis and pharmacological evaluation of analogues of benzyl quinolone

carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the

M ₁ muscarinic acetylcholine receptor. J Med Chem. 2014 Jun 26;57(12):5405-18.

doi: 10.1021/jm500556a. Epub 2014 Jun 5. PubMed PMID: 24856614.

3: Mistry SN, Valant C, Sexton PM, Capuano B, Christopoulos A, Scammells PJ.

Synthesis and pharmacological profiling of analogues of benzyl quinolone

carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor. J

Med Chem. 2013 Jun 27;56(12):5151-72. doi: 10.1021/jm400540b. Epub 2013 Jun 17.

PubMed PMID: 23718562.

Original: UNC-926 free base 1184136-10-4, stock more than 100g

2018 CHINA CPHI, W4E82

Description: UNC-926 is a L3MBTL1 domain inhibitor. UNC-926 binds to the MBT domain of the L3MBTL1 protein (Kd = 3.9 μM).

Name: UNC-926 free base

CAS#: 1184136-10-4 (free base)

Chemical Formula: C16H21BrN2O

Exact Mass: 336.0837

Molecular Weight: 337.261

Elemental Analysis: C, 56.98; H, 6.28; Br, 23.69; N, 8.31; O, 4.74

Related CAS #: 1782573-49-2 (HCl) 1184136-10-4 (free base) 1581296-53-8 (TFA)

Synonym: UNC-926 free base; UNC-926; UNC926; UNC 926.

IUPAC/Chemical Name: (3-Bromophenyl)[4-(1-pyrrolidinyl)-1-piperidinyl]methanone

InChi Key: OWGLFIKZKQOYHZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H21BrN2O/c17-14-5-3-4-13(12-14)16(20)19-10-6-15(7-11-19)18-8-1-2-9-18/h3-5,12,15H,1-2,6-11H2

SMILES Code: O=C(C1=CC=CC(Br)=C1)N2CCC(N3CCCC3)CC2

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: Zhou H, Che X, Bao G, Wang N, Peng L, Barnash KD, Frye SV, James LI, Bai X.

Design, synthesis, and protein methyltransferase activity of a unique set of

constrained amine containing compounds. Bioorg Med Chem Lett. 2016 Sep

15;26(18):4436-4440. doi: 10.1016/j.bmcl.2016.08.004. Epub 2016 Aug 3. PubMed

PMID: 27528434; PubMed Central PMCID: PMC4996710.

Original: KPT-9274 1643913-93-2, stock more than 100g

2018 CHINA CPHI, W4E82

Description: KPT-9274, also known as PAK4-IN-1, is a potent, selective and dual PAK4/NAMPT inhibitor. KPT-9274 interferences with PAK4/NAMPT signaling pathways, which results in reduction of G2-M transit as well as induction of apoptosis and decrease in cell invasion and migration in several human RCC cell lines. Mechanistic studies demonstrate that inhibition of the PAK4 pathway by KPT-9274 attenuates nuclear β-catenin as well as the Wnt/β-catenin targets cyclin D1 and c-Myc. KPT-9274 demonstrated the expected on-target effects in this mouse model. KPT-9274 is being evaluated in a phase I human clinical trial in solid tumors and lymphomas, which will allow this data to be rapidly translated into the clinic for the treatment of RCC.

Name: KPT-9274

CAS#: 1643913-93-2

Chemical Formula: C35H29F3N4O3

Exact Mass: 610.2192

Molecular Weight: 610.6372

Elemental Analysis: C, 68.84; H, 4.79; F, 9.33; N, 9.18; O, 7.86

Synonym: KPT-9274; KPT9274; KPT 9274; PAK4-IN-1; PAK4-IN 1; PAK4-IN1.

IUPAC/Chemical Name: (1Z,2E)-3-(6-aminopyridin-2-yl)-N-((5-(4-(4,4-difluoropiperidine-1-carbonyl)phenyl)-7-(4-fluorophenyl)benzofuran-2-yl)methyl)acrylimidic acid

InChi Key: KXGUHCDGIDAEIP-OUKQBFOZSA-N

InChi Code: InChI=1S/C35H29F3N4O3/c36-27-10-8-23(9-11-27)30-20-25(22-4-6-24(7-5-22)34(44)42-16-14-35(37,38)15-17-42)18-26-19-29(45-33(26)30)21-40-32(43)13-12-28-2-1-3-31(39)41-28/h1-13,18-20H,14-17,21H2,(H2,39,41)(H,40,43)/b13-12+

SMILES Code: OC(/C=C/C1=NC(N)=CC=C1)=N\CC2=CC3=CC(C4=CC=C(C(N5CCC(F)(F)CC5)=O)C=C4)=CC(C6=CC=C(F)C=C6)=C3O2

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

ADDITIONAL INFORMATION

Upon administration, KPT-9274 allosterically binds to, destabilizes and causes degradation of PAK4. This inhibits PAK4-mediated signaling, induces cell death in, and inhibits the proliferation of PAK4-overexpressing tumor cells. In addition, KPT-9274 binds to and inhibits the activity of NAMPT. This depletes cellular NAD and inhibits NAD-dependent enzymes, both of which are needed for rapid cell proliferation; this results in tumor cell death in NAMPT-overexpressing cancer cells. PAK4, a serine/threonine kinase and member of the PAK family of proteins upregulated in various cancer cell types, regulates cell motility, proliferation and survival. NAMPT, an enzyme that is responsible for maintaining the intracellular NAD pool, plays a key role in the regulation of cellular metabolism and has cytokine-like activities. NAMPT is often overexpressed in a variety of cancers and metabolic disorders and tumor cells rely on NAMPT activity for their NAD supply.

REFERENCES

1: Rane C, Senapedis W, Baloglu E, Landesman Y, Crochiere M, Das-Gupta S, Minden A. A novel orally bioavailable compound KPT-9274 inhibits PAK4, and blocks triple negative breast cancer tumor growth. Sci Rep. 2017 Feb 15;7:42555. doi: 10.1038/srep42555. PubMed PMID: 28198380.

2: Fulciniti M, Martinez-Lopez J, Senapedis W, Oliva S, Bandi RL, Amodio N, Xu Y, Szalat RL, Gulla A, Samur MK, Roccaro A, Linares M, Cea M, Baloglu E, Argueta C, Landesman Y, Shacham S, Liu S, Schenone M, Wu SL, Karger B, Prabhala R, Anderson KC, Munshi NC. Functional role and therapeutic targeting of p21-associated kinase 4 (PAK4) in multiple myeloma. Blood. 2017 Jan 17. pii: blood-2016-06-724831. doi: 10.1182/blood-2016-06-724831. [Epub ahead of print] PubMed PMID: 28096095.

3: Aboukameel A, Muqbil I, Senapedis W, Baloglu E, Landesman Y, Shacham S, Kauffman M, Philip PA, Mohammad RM, Azmi AS. Novel p21-Activated Kinase 4 (PAK4) Allosteric Modulators Overcome Drug Resistance and Stemness in Pancreatic Ductal Adenocarcinoma. Mol Cancer Ther. 2017 Jan;16(1):76-87. doi: 10.1158/1535-7163.MCT-16-0205. PubMed PMID: 28062705; PubMed Central PMCID: PMC5221563.

4: Abu Aboud O, Chen CH, Senapedis W, Baloglu E, Argueta C, Weiss RH. Dual and Specific Inhibition of NAMPT and PAK4 By KPT-9274 Decreases Kidney Cancer Growth. Mol Cancer Ther. 2016 Sep;15(9):2119-29. doi: 10.1158/1535-7163.MCT-16-0197. PubMed PMID: 27390344; PubMed Central PMCID: PMC5010932.

Original: LY3009120 1454682-72-4, stock more than 100g

2018 CHINA CPHI, W4E82

Description: LY3009120, also known as DP-4978, is potent and selective pan-RAF inhibitor with potential anticancer activity. LY3009120 showed activities against BRaf or Ras mutant tumor cells . LY3009120 binds to ARaf, BRaf and CRaf isoforms with similar affinity in cells with activating mutations of BRaf or KRas. LY3009120 induces minimal paradoxical pathway activation in NRas or KRas mutant cells. LY3009120 inhibits MEK phosphorylation and cell proliferation in vitro, and exhibits anti-tumor activity in multiple xenograft models carrying mutations in BRaf, NRas or KRas.

Name: LY3009120

CAS#: 1454682-72-4

Chemical Formula: C23H29FN6O

Exact Mass: 424.23869

Molecular Weight: 424.52

Elemental Analysis: C, 65.07; H, 6.89; F, 4.48; N, 19.80; O, 3.77

Synonym: LY3009120; LY-3009120; LY 3009120; DP4978; DP 4978; DP-4978.

IUPAC/Chemical Name: 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea

InChi Key: HHCBMISMPSAZBF-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H29FN6O/c1-13-9-18(24)19(29-22(31)26-8-7-23(3,4)5)11-16(13)17-10-15-12-27-21(25-6)30-20(15)28-14(17)2/h9-12H,7-8H2,1-6H3,(H2,26,29,31)(H,25,27,28,30)

SMILES Code: O=C(NC1=CC(C2=CC3=CN=C(NC)N=C3N=C2C)=C(C)C=C1F)NCCC(C)(C)C

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

LY3009120 is a potentially best-in-class inhibitor of three Raf isoforms and Raf dimer, with activity against tumor cells with BRaf, NRas or KRas mutations, as well as melanoma cells with acquired resistance to current BRaf therapies.

Original: GNE-3511 1496581-76-0, stock more than 100g

2018 CHINA CPHI, W4E82

Description: GNE-3511 is a potent and selective dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models. GNE-3511 displays concentration-dependent protection of neurons from degeneration in vitro and demonstrated dose-dependent activity in two different animal models of disease. GNE-3511 displays protection of primary neurons in an in vitro axon degeneration assay as well as activity in the mouse models of glaucoma/optic neuropathy (optic nerve crush) and Parkinson’s disease (MPTP) after oral dosing.

Name: GNE-3511

CAS#: 1496581-76-0

Chemical Formula: C23H26F2N6O

Exact Mass: 440.21362

Molecular Weight: 440.5

Elemental Analysis: C, 62.71; H, 5.95; F, 8.63; N, 19.08; O, 3.63

Synonym: GNE-3511; GNE 3511; GNE3511.

IUPAC/Chemical Name: 2-((6-(3,3-difluoropyrrolidin-1-yl)-4-(1-(oxetan-3-yl)piperidin-4-yl)pyridin-2-yl)amino)isonicotinonitrile

InChi Key: RHFIAUKMKYHHFA-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H26F2N6O/c24-23(25)4-8-31(15-23)22-11-18(17-2-6-30(7-3-17)19-13-32-14-19)10-21(29-22)28-20-9-16(12-26)1-5-27-20/h1,5,9-11,17,19H,2-4,6-8,13-15H2,(H,27,28,29)

SMILES Code: N#CC1=CC(NC2=NC(N3CC(F)(F)CC3)=CC(C4CCN(C5COC5)CC4)=C2)=NC=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

REFERENCES

1: Patel S, Cohen F, Dean BJ, De La Torre K, Deshmukh G, Estrada AA, Ghosh AS, Gibbons P, Gustafson A, Huestis MP, Le Pichon CE, Lin H, Liu W, Liu X, Liu Y, Ly CQ, Lyssikatos JP, Ma C, Scearce-Levie K, Shin YG, Solanoy H, Stark KL, Wang J, Wang B, Zhao X, Lewcock JW, Siu M. Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models. J Med Chem. 2015 Jan 8;58(1):401-18. doi: 10.1021/jm5013984. Epub 2014 Oct 23. PubMed PMID: 25341110.

Original:HMN-154 173528-92-2, stock more than 100g

2018 CHINA CPHI, W4E82

Description: HMN-154 is a benzenesulfonamide anticancer agent. HMN-154 inhibits DNA binding of NF-Y to the human major histocompatibility complex class II human leukocyte antigen DRA Y-box sequence in a dose-dependent manner.

Name: HMN-154

CAS#: 173528-92-2

Chemical Formula: C20H18N2O3S

Exact Mass: 366.1038

Molecular Weight: 366.435

Elemental Analysis: C, 65.56; H, 4.95; N, 7.65; O, 13.10; S, 8.75

Synonym: HMN-154; HMN 154; HMN154.

IUPAC/Chemical Name: (E)-4-(2-(2-(N-(4-Methoxybenzenesulfonyl)amino)phenyl)ethenyl)pyridine

InChi Key: CIJCDFMGZYKSSC-VOTSOKGWSA-N

InChi Code: InChI=1S/C20H18N2O3S/c1-25-18-8-10-19(11-9-18)26(23,24)22-20-5-3-2-4-17(20)7-6-16-12-14-21-15-13-16/h2-15,22H,1H3/b7-6+

SMILES Code: O=S(NC1=CC=CC=C1/C=C/C2=CC=NC=C2)(C3=CC=C(OC)C=C3)=O

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: Tanaka H, Ohshima N, Hidaka H. Isolation of cDNAs encoding cellular

drug-binding proteins using a novel expression cloning procedure: drug-western.

Mol Pharmacol. 1999 Feb;55(2):356-63. PubMed PMID: 9927629.

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2018年5月6日星期日

Original:ML130 799264-47-4 , stock more than 100g

Original: AA26-9 1312782-34-5 , stock more than 100g

Original:BQCA 338747-41-4 , stock more than 100g

Original: UNC-926 free base 1184136-10-4, stock more than 100g

Original: KPT-9274 1643913-93-2, stock more than 100g

Original: LY3009120 1454682-72-4, stock more than 100g

Original: GNE-3511 1496581-76-0, stock more than 100g

Original:HMN-154 173528-92-2, stock more than 100g

举报滥用情况

2016 China CPHI meet