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    Everolimus solution

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      Everolimus solution, 1.0 mg/ml in acetonitrile

      SKU
      E0574

      Category: API's & Intermediates

      Synonyms
      42-O-(2-Hydroxyethyl)rapamycin , NVP-RAD001 , RAD001 , SDZRAD , Zortress , Afinitor , Certican , Votubia
      159351-69-6
      CAS-Number
      C53H83NO14
      Molecular Formula
      958.22
      Molecular Weight

      • Product Data
      • Handling
      • Safety Information
      • Details

      Specifications

      Purity
      ≥99% (HPLC)
      Identity
      IR
      Appearance
      Liquid
      Concentration
      1.0 mg/ml in acetonitrile

      Properties

      Use / Stability
      Stable for at least 2 years after receipt when stored at -20°C.
      Handling Advice
      Protect from light and moisture.
      Long Term Storage
      -20°C
      Short Term Storage
      -20°C
      Shipping
      AMBIENT
      Transportation
      Packing Group II
      RIDADR
      1648 3
      Signal word
      Danger
      Precautionary statements
      P210-P305 + P351 + P338
      Hazard statements
      H225-H302 + H332-H319
      Description
      Macrolide antibiotic, inhibiting bacterial protein synthesis. Potent immunosuppressant. Binds with high affinity to the FK506 binding protein-12 (FKBP-12) to generate an immunosuppressive complex that inhibits the activation of the mammalian target of rapamycin (mTOR). More selective for the mTORC1 protein complex, with little impact on the mTORC2 complex, compared to Rapamycin. Anticancer agent. Inhibition of mTOR reduces the activity of effectors downstream, which leads to a blockage in the progression of cells from G1 into S phase, and subsequently inducing cell growth arrest, apoptosis and autophagy, resulting in reduction of cell proliferation, angiogenesis and glucose uptake. Inhibits tumor proliferation in vitro and in vivo. This compound can be used as a reference material.
      InChi
      InChI=1S/C53H83NO14/c1-32-16-12-11-13-17-33(2)44(63-8)30-40-21-19-38(7)53(62,68-40)50(59)51(60)54-23-15-14-18-41(54)52(61)67-45(35(4)28-39-20-22-43(66-25-24-55)46(29-39)64-9)31-42(56)34(3)27-37(6)48(58)49(65-10)47(57)36(5)26-32/h11-13,16-17,27,32,34-
      References
      (1) H.J. Schuurman, et al., Transplantation 64, 32 (1997) , (2) W. Schuler, et al., Transplantation 64, 36 (1997) , (3) P. Neuhaus, et al., Liver Transpl. 7, 473 (2001) (Review) , (4) B. Nashan, Expert Opin. Investig. Drugs. 11, 1845 (2002) (Review) , (5) I. Beuvink, et al., Cell 120, 747 (2005) , (6) J.K. Patel & J.A. Kobashigawa, Expert Opin. Pharmacother. 7, 1347 (2006) (Review) , (7) P. Smolewski, Anticancer Drugs 17, 487 (2006) (Review) , (8) K. Zitzmann, et al., Neuroendocrinology 85, 54 (2007) , (9) Z. Zeng, et al., Blood 109, 3509 (2007) , (10) R. Bianco, et al., Br. J. Cancer 98, 923 (2008) , (11) A.I. Sanchez-Fructuoso, Expert Opin. Drug Metab. Toxicol. 4, 807 (2008) (Review) , (12) H.A. Lane, et al., Clin. Cancer Res. 15, 1612 (2009) , (13) D. Lebwohl, et al., Ann. N. Y. Acad. Sci. 1291, 14 (2013) (Review) , (14) U. Saran, et al., Clin. Sci. 129, 895 (2015) (Review) , (15) Morviducci, et al., Diabetes Res. Clin. Pract. (Epub ahead of print) (2018) (Review)
      InChi Key
      HKVAMNSJSFKALM-QATPHWSPSA-N
      Smiles
      OCCO[C@H]1[C@H](OC)C[C@H](C[C@@H](C)[C@H](CC([C@H](C)/C=C(C)/[C@@H](O)[C@H]2OC)=O)OC([C@@H]3CCCCN3C(C([C@@]4(O)[C@H](C)CC[C@@H](C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C2=O)O4)=O)=O)=O)CC1

      Macrolide antibiotic, inhibiting bacterial protein synthesis. Potent immunosuppressant. Binds with high affinity to the FK506 binding protein-12 (FKBP-12) to generate an immunosuppressive complex that inhibits the activation of the mammalian target of rapamycin (mTOR). More selective for the mTORC1 protein complex, with little impact on the mTORC2 complex, compared to Rapamycin. Anticancer agent. Inhibition of mTOR reduces the activity of effectors downstream, which leads to a blockage in the progression of cells from G1 into S phase, and subsequently inducing cell growth arrest, apoptosis and autophagy, resulting in reduction of cell proliferation, angiogenesis and glucose uptake. Inhibits tumor proliferation in vitro and in vivo. This compound can be used as a reference material.

      SKU: E0574 Category: API's & Intermediates
      • Additional information

      Additional information

      Synonyms

      42-O-(2-Hydroxyethyl)rapamycin, NVP-RAD001, RAD001, SDZRAD, Zortress, Afinitor, Certican, Votubia

      Purity

      ≥99% (HPLC)

      Appearance

      Liquid

      CAS-Number

      159351-69-6

      Molecular Formula

      C53H83NO14

      Molecular Weight

      958.22

      Identity

      IR

      Smiles

      OCCO[C@H]1[C@H](OC)C[C@H](C[C@@H](C)[C@H](CC([C@H](C)/C=C(C)/[C@@H](O)[C@H]2OC)=O)OC([C@@H]3CCCCN3C(C([C@@]4(O)[C@H](C)CC[C@@H](C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C2=O)O4)=O)=O)=O)CC1

      InChi Key

      HKVAMNSJSFKALM-QATPHWSPSA-N

      Shipping

      AMBIENT

      Short Term Storage

      -20°C

      Long Term Storage

      -20°C

      Handling Advice

      Protect from light and moisture.

      Use / Stability

      Stable for at least 2 years after receipt when stored at -20°C.

      Hazard statements

      H225-H302 + H332-H319

      Precautionary statements

      P210-P305 + P351 + P338

      Signal word

      Danger

      RIDADR

      1648 3

      Transportation

      Packing Group II

      References

      (1) H.J. Schuurman, et al., Transplantation 64, 32 (1997), (2) W. Schuler, et al., Transplantation 64, 36 (1997), (3) P. Neuhaus, et al., Liver Transpl. 7, 473 (2001) (Review), (4) B. Nashan, Expert Opin. Investig. Drugs. 11, 1845 (2002) (Review), (5) I. Beuvink, et al., Cell 120, 747 (2005), (6) J.K. Patel & J.A. Kobashigawa, Expert Opin. Pharmacother. 7, 1347 (2006) (Review), (7) P. Smolewski, Anticancer Drugs 17, 487 (2006) (Review), (8) K. Zitzmann, et al., Neuroendocrinology 85, 54 (2007), (9) Z. Zeng, et al., Blood 109, 3509 (2007), (10) R. Bianco, et al., Br. J. Cancer 98, 923 (2008), (11) A.I. Sanchez-Fructuoso, Expert Opin. Drug Metab. Toxicol. 4, 807 (2008) (Review), (12) H.A. Lane, et al., Clin. Cancer Res. 15, 1612 (2009), (13) D. Lebwohl, et al., Ann. N. Y. Acad. Sci. 1291, 14 (2013) (Review), (14) U. Saran, et al., Clin. Sci. 129, 895 (2015) (Review), (15) Morviducci, et al., Diabetes Res. Clin. Pract. (Epub ahead of print) (2018) (Review)

      InChi

      InChI=1S/C53H83NO14/c1-32-16-12-11-13-17-33(2)44(63-8)30-40-21-19-38(7)53(62,68-40)50(59)51(60)54-23-15-14-18-41(54)52(61)67-45(35(4)28-39-20-22-43(66-25-24-55)46(29-39)64-9)31-42(56)34(3)27-37(6)48(58)49(65-10)47(57)36(5)26-32/h11-13,16-17,27,32,34-

      Quantity

      1 ml, Bulk

      cdx-Concentration

      1.0 mg/ml in acetonitrile

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