EOS Med Chem, Medicinal Chemical is Big

2018年5月1日星期二

Original: Epacadostat 1204669-58-8 , 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
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Description: Epacadostat, also known as INCB024360 or INCB24360, is an orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase (IDO1), with potential immunomodulating and antineoplastic activities. INCB024360 targets and binds to IDO1, an enzyme responsible for the oxidation of tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, INCB024360 increases and restores the proliferation and activation of various immune cells, including dendritic cells (DCs), NK cells, and T-lymphocytes, as well as interferon (IFN) production, and a reduction in tumor-associated regulatory T cells (Tregs).

Name: Epacadostat (INCB024360)

CAS#: 1204669-58-8 (INCB024360)

Chemical Formula: C11H13BrFN7O4S

Exact Mass: 436.99171

Molecular Weight: 438.23

Elemental Analysis: C, 30.15; H, 2.99; Br, 18.23; F, 4.34; N, 22.37; O, 14.60; S, 7.32

Related CAS #: 1204669-58-8 (INCB024360) 1204669-37-3 (INCB024360) 914471-09-3 (INCB024360-analog)

Synonym: INCB024360; INCB 024360; INCB-024360; INCB24360; INCB-24360; INCB 24360; Epacadostat

IUPAC/Chemical Name: (Z)-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-((2-(sulfamoylamino)ethyl)amino)-1,2,5-oxadiazole-3-carboximidamide

InChi Key: FBKMWOJEPMPVTQ-UHFFFAOYSA-N

InChi Code: InChI=1S/C11H13BrFN7O4S/c12-7-5-6(1-2-8(7)13)17-11(18-21)9-10(20-24-19-9)15-3-4-16-25(14,22)23/h1-2,5,16,21H,3-4H2,(H,15,20)(H,17,18)(H2,14,22,23)

SMILES Code: O=S(NCCNC1=NON=C1/C(NC2=CC=C(F)C(Br)=C2)=N/O)(N)=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, DMA, etc. Method 1: INCB024360 was reconstituted in 5% DMA, 47.5% propylene glycol. (See J. Med. Chem, 2009, 52(23), 7364. supporting information). Methdod 2: INCB024360 was reconstituted in 3% DMA, 10% (2-Hydroxypropyl) β-Cyclodextrin. (see: Mol. Cancer. Ther. 2010, 9(2), 489. ). Note: DMA = N,N–Dimethylacetamide.

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

Related CAS#:

INCB024360: CAS#1204669-58-8 (or 1204669-37-3)

INCB024360-analog: CAS#914471-09-3

REFERENCES

1: Yue EW, Sparks R, Polam P, Modi D, Douty B, Wayland B, Glass B, Takvorian A, Glenn J, Zhu W, Bower M, Liu X, Leffet L, Wang Q, Bowman KJ, Hansbury MJ, Wei M, Li Y, Wynn R, Burn TC, Koblish HK, Fridman JS, Emm T, Scherle PA, Metcalf B, Combs AP. INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology. ACS Med Chem Lett. 2017 Mar 6;8(5):486-491. doi: 10.1021/acsmedchemlett.6b00391. eCollection 2017 May 11. PubMed PMID: 28523098; PubMed Central PMCID: PMC5430407.

2: Wu Y, Xu T, Liu J, Ding K, Xu J. Structural insights into the binding mechanism of IDO1 with hydroxylamidine based inhibitor INCB14943. Biochem Biophys Res Commun. 2017 May 27;487(2):339-343. doi: 10.1016/j.bbrc.2017.04.061. Epub 2017 Apr 13. PubMed PMID: 28412361.

3: Maliniemi P, Laukkanen K, Väkevä L, Dettmer K, Lipsanen T, Jeskanen L, Bessede A, Oefner PJ, Kadin ME, Ranki A. Biological and clinical significance of tryptophan-catabolizing enzymes in cutaneous T-cell lymphomas. Oncoimmunology. 2017 Feb 10;6(3):e1273310. doi: 10.1080/2162402X.2016.1273310. eCollection 2017. PubMed PMID: 28405495; PubMed Central PMCID: PMC5384345.

4: Brochez L, Chevolet I, Kruse V. The rationale of indoleamine 2,3-dioxygenase inhibition for cancer therapy. Eur J Cancer. 2017 May;76:167-182. doi: 10.1016/j.ejca.2017.01.011. Epub 2017 Mar 18. Review. PubMed PMID: 28324751.

5: Zhang Q, Zhang Y, Boer J, Shi JG, Hu P, Diamond S, Yeleswaram S. In Vitro Interactions of Epacadostat and its Major Metabolites with Human Efflux and Uptake Transporters: Implications for Pharmacokinetics and Drug Interactions. Drug Metab Dispos. 2017 Jun;45(6):612-623. doi: 10.1124/dmd.116.074609. Epub 2017 Mar 10. PubMed PMID: 28283500.

6: Beatty GL, O'Dwyer PJ, Clark J, Shi JG, Bowman KJ, Scherle PA, Newton RC, Schaub R, Maleski J, Leopold L, Gajewski TF. First-in-Human Phase I Study of the Oral Inhibitor of Indoleamine 2,3-Dioxygenase-1 Epacadostat (INCB024360) in Patients with Advanced Solid Malignancies. Clin Cancer Res. 2017 Jan 4. doi: 10.1158/1078-0432.CCR-16-2272. [Epub ahead of print] PubMed PMID: 28053021.

7: Shi JG, Bowman KJ, Chen X, Maleski J, Leopold L, Yeleswaram S. Population Pharmacokinetic and Pharmacodynamic Modeling of Epacadostat in Patients With Advanced Solid Malignancies. J Clin Pharmacol. 2017 Jun;57(6):720-729. doi: 10.1002/jcph.855. Epub 2016 Dec 19. PubMed PMID: 27990653.

8: Jochems C, Fantini M, Fernando RI, Kwilas AR, Donahue RN, Lepone LM, Grenga I, Kim YS, Brechbiel MW, Gulley JL, Madan RA, Heery CR, Hodge JW, Newton R, Schlom J, Tsang KY. The IDO1 selective inhibitor epacadostat enhances dendritic cell immunogenicity and lytic ability of tumor antigen-specific T cells. Oncotarget. 2016 Jun 21;7(25):37762-37772. doi: 10.18632/oncotarget.9326. PubMed PMID: 27192116; PubMed Central PMCID: PMC5122347.

9: Boer J, Young-Sciame R, Lee F, Bowman KJ, Yang X, Shi JG, Nedza FM, Frietze W, Galya L, Combs AP, Yeleswaram S, Diamond S. Roles of UGT, P450, and Gut Microbiota in the Metabolism of Epacadostat in Humans. Drug Metab Dispos. 2016 Oct;44(10):1668-74. doi: 10.1124/dmd.116.070680. Epub 2016 Jul 25. PubMed PMID: 27457784.

10: Dhiman V, Giri KK, S SP, Zainuddin M, Rajagopal S, Mullangi R. Determination of epacadostat, a novel IDO1 inhibitor in mouse plasma by LC-MS/MS and its application to a pharmacokinetic study in mice. Biomed Chromatogr. 2017 Feb;31(2). doi: 10.1002/bmc.3794. Epub 2016 Aug 11. PubMed PMID: 27451018.

11: Shi JG, Chen X, Punwani NG, Williams WV, Yeleswaram S. Potential Underprediction of Warfarin Drug Interaction From Conventional Interaction Studies and Risk Mitigation: A Case Study With Epacadostat, an IDO1 Inhibitor. J Clin Pharmacol. 2016 Nov;56(11):1344-1354. doi: 10.1002/jcph.737. PubMed PMID: 26990117.

12: Zhai L, Spranger S, Binder DC, Gritsina G, Lauing KL, Giles FJ, Wainwright DA. Molecular Pathways: Targeting IDO1 and Other Tryptophan Dioxygenases for Cancer Immunotherapy. Clin Cancer Res. 2015 Dec 15;21(24):5427-33. doi: 10.1158/1078-0432.CCR-15-0420. Epub 2015 Oct 30. Review. PubMed PMID: 26519060; PubMed Central PMCID: PMC4681601.

13: Vacchelli E, Aranda F, Eggermont A, Sautès-Fridman C, Tartour E, Kennedy EP, Platten M, Zitvogel L, Kroemer G, Galluzzi L. Trial watch: IDO inhibitors in cancer therapy. Oncoimmunology. 2014 Dec 15;3(10):e957994. eCollection 2014 Nov. Review. PubMed PMID: 25941578; PubMed Central PMCID: PMC4292223.

14: Liu X, Shin N, Koblish HK, Yang G, Wang Q, Wang K, Leffet L, Hansbury MJ, Thomas B, Rupar M, Waeltz P, Bowman KJ, Polam P, Sparks RB, Yue EW, Li Y, Wynn R, Fridman JS, Burn TC, Combs AP, Newton RC, Scherle PA. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood. 2010 Apr 29;115(17):3520-30. doi: 10.1182/blood-2009-09-246124. Epub 2010 Mar 2. PubMed PMID: 20197554.

15: Koblish HK, Hansbury MJ, Bowman KJ, Yang G, Neilan CL, Haley PJ, Burn TC, Waeltz P, Sparks RB, Yue EW, Combs AP, Scherle PA, Vaddi K, Fridman JS. Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors. Mol Cancer Ther. 2010 Feb;9(2):489-98. doi: 10.1158/1535-7163.MCT-09-0628. Epub 2010 Feb 2. PubMed PMID: 20124451.

Original: ALG1001 1307293-62-4 , stock more than 100g

2018 CHINA CPHI, W4E82

Description: ALG1001 is an angiogenesis inhibitors and Integrin alpha 5 beta 1 modulator. ALG1001 targets integrin alpha2beta1, alphaV-beta 3, alphaV-beta 5. ALG1001 is being developed by Allegro Ophthalmics. ALG1001 has been shown to be effective at regressing and inhibiting new blood vessel formation, as well as reducing vascular leakage to maintain and restore vision.

Name: ALG1001

CAS#: 1307293-62-4

Chemical Formula: C22H39N9O11S

Exact Mass: 637.249

Molecular Weight: 637.666

Elemental Analysis: C, 41.44; H, 6.16; N, 19.77; O, 27.60; S, 5.03

Synonym: ALG1001; ALG-1001; ALG 1001; Luminate; H-Gly-Arg-Gly-（L-Ala（SO3））-Thr-Pro-OH.

IUPAC/Chemical Name: L-Proline, glycyl-L-arginylglycyl-3-sulfo-L-alanyl-L-threonyl-

InChi Key: MYZAXBZLEILEBR-RVFOSREFSA-N

InChi Code: InChI=1S/C22H39N9O11S/c1-11(32)17(20(37)31-7-3-5-14(31)21(38)39)30-19(36)13(10-43(40,41)42)29-16(34)9-27-18(35)12(28-15(33)8-23)4-2-6-26-22(24)25/h11-14,17,32H,2-10,23H2,1H3,(H,27,35)(H,28,33)(H,29,34)(H,30,36)(H,38,39)(H4,24,25,26)(H,40,41,42)/t11-,12+,13+,14+,17+/m1/s1

SMILES Code: O=C(O)[C@H]1N(C([C@H]([C@H](O)C)NC([C@H](CS(=O)(O)=O)NC(CNC([C@H](CCCNC(N)=N)NC(CN)=O)=O)=O)=O)=O)CCC1

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. Mackel, Michael John; Park, John Y.; Karageozian, Hampar L.; Karageozian, Vicken H. Integrin receptor antagonists and their methods of use. U.S. Pat. Appl. Publ. (2013), US 20130129621 A1 20130523.

2. Mackel, Michael John; Park, John Y.; Karageozian, Hampar L.; Karageozian, Vicken H. Integrin receptor antagonists and their methods of use. PCT Int. Appl. (2012), WO 2012154894 A2 20121115.

3. Mackel, Michael John; Park, John Compositions and methods for inhibiting cellular adhesion or directing diagnostic or therapeutic agents to rgd binding sites. PCT Int. Appl. (2011), WO 2011060104 A2 20110519.

Original: T-5224 530141-72-1 , stock more than 100g

2018 CHINA CPHI, W4E82

Description: T-5224 is a selective inhibitor of c-Fos/activator protein-1. T-5224 ameliorates liver injury and improves survival through decreasing production of proinflammatory cytokines and chemokines in endotoxemic mice. T-5224 has been investigated in phase II human clinical trials. T-5224 may be a promising new treatment for septic kidney injury. Activator protein 1 (AP-1) is a pivotal transcription factor that regulates a wide range of cellular processes including proliferation, apoptosis, differentiation, survival, cell migration, and transformation.

Name: T-5224

CAS#: 530141-72-1

Chemical Formula: C29H27NO8

Exact Mass: 517.17367

Molecular Weight: 517.52658

Elemental Analysis: C, 67.30; H, 5.26; N, 2.71; O, 24.73

Synonym: T5224, T-5224, T 5224

IUPAC/Chemical Name: 3-(5-(4-(cyclopentyloxy)-2-hydroxybenzoyl)-2-((3-hydroxybenzo[d]isoxazol-6-yl)methoxy)phenyl)propanoic acid

InChi Key: DALCQQSLNPLQFZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H27NO8/c31-24-15-21(37-20-3-1-2-4-20)8-10-22(24)28(34)19-6-11-25(18(14-19)7-12-27(32)33)36-16-17-5-9-23-26(13-17)38-30-29(23)35/h5-6,8-11,13-15,20,31H,1-4,7,12,16H2,(H,30,35)(H,32,33)

SMILES Code: O=C(O)CCC1=CC(C(C2=CC=C(OC3CCCC3)C=C2O)=O)=CC=C1OCC4=CC5=C(C=C4)C(O)=NO5

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: Ye N, Ding Y, Wild C, Shen Q, Zhou J. Small Molecule Inhibitors Targeting Activator Protein 1 (AP-1). J Med Chem. 2014 Aug 28;57(16):6930-48. doi: 10.1021/jm5004733. Epub 2014 May 27. PubMed PMID: 24831826; PubMed Central PMCID: PMC4148154.

2: Miyazaki H, Morishita J, Ueki M, Nishina K, Shiozawa S, Maekawa N. The effects of a selective inhibitor of c-Fos/activator protein-1 on endotoxin-induced acute kidney injury in mice. BMC Nephrol. 2012 Nov 23;13:153. doi: 10.1186/1471-2369-13-153. PubMed PMID: 23173923; PubMed Central PMCID: PMC3557146.

3: Izuta S, Ueki M, Ueno M, Nishina K, Shiozawa S, Maekawa N. T-5224, a selective inhibitor of c-Fos/activator protein-1, attenuates lipopolysaccharide-induced liver injury in mice. Biotechnol Lett. 2012 Dec;34(12):2175-82. doi: 10.1007/s10529-012-1022-4. Epub 2012 Aug 25. PubMed PMID: 22927112.

4: Avouac J, Palumbo K, Tomcik M, Zerr P, Dees C, Horn A, Maurer B, Akhmetshina A, Beyer C, Sadowski A, Schneider H, Shiozawa S, Distler O, Schett G, Allanore Y, Distler JH. Inhibition of activator protein 1 signaling abrogates transforming growth factor β-mediated activation of fibroblasts and prevents experimental fibrosis. Arthritis Rheum. 2012 May;64(5):1642-52. doi: 10.1002/art.33501. PubMed PMID: 22139817.

5: Uchihashi S, Fukumoto H, Onoda M, Hayakawa H, Ikushiro S, Sakaki T. Metabolism of the c-Fos/activator protein-1 inhibitor T-5224 by multiple human UDP-glucuronosyltransferase isoforms. Drug Metab Dispos. 2011 May;39(5):803-13. doi: 10.1124/dmd.110.037952. Epub 2011 Feb 23. PubMed PMID: 21346002.

Original: BAY-1895344 1876467-74-1 , stock more than 100g

2018 CHINA CPHI, W4E82

Description: BAY-1895344 is a potent and selective ATM inhibitor. BAY 1895344 shows potent anti-tumor efficacy in monotherapy and strong combination potential with the targeted alpha therapy Radium-223 dichloride.

Name: BAY-1895344 HCl

CAS#: 1876467-74-1 (free base)

Chemical Formula: C20H22ClN7O

Exact Mass: 375.1808

Molecular Weight: 411.89

Elemental Analysis: C, 58.32; H, 5.38; Cl, 8.61; N, 23.80; O, 3.88

Related CAS #: 1876467-74-1 (free base) Note: CAS# for BAY-1895344 HCl is unknown

Synonym: BAY-1895344; BAY 1895344; BAY1895344.

IUPAC/Chemical Name: (R)-3-methyl-4-(4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-5-yl)-1,7-naphthyridin-2-yl)morpholine hydrochloride

InChi Key: KWQNBYGUBHMRPY-BTQNPOSSSA-N

InChi Code: InChI=1S/C20H21N7O.ClH/c1-13-12-28-10-9-27(13)18-11-15(17-5-8-23-26(17)2)14-3-6-21-20(19(14)24-18)16-4-7-22-25-16;/h3-8,11,13H,9-10,12H2,1-2H3,(H,22,25);1H/t13-;/m1./s1

SMILES Code: CN1N=CC=C1C2=CC(N3[C@H](C)COCC3)=NC4=C(C5=CC=NN5)N=CC=C24.[H]Cl

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

Original: GSK-5959 901245-65-6 , stock more than 100g

2018 CHINA CPHI, W4E82

Description: GSK-5959 is a potent and selective BRPF1 bromodomain inhibitor (IC50 = 80 nM). GSK-5959 exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains. BRPF1 (bromodomain and PHD finger containing protein 1) is involved in the epigenetic regulation of gene expression and have been implicated in human cancer.

Name: GSK-5959

CAS#: 901245-65-6

Chemical Formula: C22H26N4O3

Exact Mass: 394.20049

Molecular Weight: 394.48

Elemental Analysis: C, 66.99; H, 6.64; N, 14.20; O, 12.17

Synonym: GSK-5959; GSK 5959; GSK5959.

IUPAC/Chemical Name: N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-piperidinyl)-1H-benzimidazol-5-yl]-2-methoxybenzamide

InChi Key: LTUGYAOMCKNTGG-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H26N4O3/c1-24-18-13-16(23-21(27)15-9-5-6-10-20(15)29-3)17(26-11-7-4-8-12-26)14-19(18)25(2)22(24)28/h5-6,9-10,13-14H,4,7-8,11-12H2,1-3H3,(H,23,27)

SMILES Code: O=C(NC1=C(N2CCCCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC

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

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2018年5月1日星期二

Original: Epacadostat 1204669-58-8 , stock more than 100g

Original: ALG1001 1307293-62-4 , stock more than 100g

Original: T-5224 530141-72-1 , stock more than 100g

Original: BAY-1895344 1876467-74-1 , stock more than 100g

Original: GSK-5959 901245-65-6 , stock more than 100g

举报滥用情况

2016 China CPHI meet