RapaLink-1

Product Name: RapaLink-1
CAS No.: 1887095-82-0
Chemical Name: RapaLink-1
Synonyms: RapaLink-1;RAPALINK 1;RAPALINK1;Rapamycin, 42-O-[2-[[1-[32-[4-amino-3-(2-amino-5-benzoxazolyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-27-oxo-3,6,9,12,15,18,21,24-octaoxa-28-azadotriacont-1-yl]-1H-1,2,3-triazol-4-yl]methoxy]ethyl]-;N-(4-(4-Amino-3-(2-aminobenzo[d]oxazol-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)butyl)-1-(4-((2-(((1R,2R,4S)-4-((R)-2-((3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-1,5,11,28,29-pentaoxo-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34a-tetracosahydro-3H-23,27-epoxypyrido[2,1-c][1]oxa[4]azacyclohentriacontin-3-yl)propyl)-2-methoxycyclohexyl)oxy)ethoxy)methyl)-1H-1,2,3-triazol-1-yl)-3,6,9,12,15,18,21,24-octaoxa;N-(4-(4-Amino-3-(2-aminobenzo[d]oxazol-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)butyl)-1-(4-((2-(((1R,2R,4S)-4-((R)-2-((3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-1,5,11,28,29-pentaoxo-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34a-tetracosahydro-3H-23,27-epoxypyrido[2,1-c][1]oxa[4]azacyclohentriacontin-3-yl)propyl)-2-methoxycyclohexyl)oxy)ethoxy)methyl)-1H-1,2,3-triazol-1-yl)-3,6,9,12,15,18,21,24-octaoxaheptacosan-27-amide
CBNumber: CB93339911
Molecular Formula: C91H138N12O24
Formula Weight: 1784.17
MOL File: 1887095-82-0.mol

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RapaLink-1 Property

Density: 1.30±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: ≥ 178.4mg/mL in DMSO
form: Solid
pka: 10.40±0.70(Predicted)
color: White to light yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0040187
Product name: RapaLink-1
Purity: ≥98.0%
Packaging: 1mg
Price: $490
Updated: 2021/12/16

ApexBio Technology

Product number: A8764
Product name: Rapalink-1
Packaging: 5mg
Price: $700
Updated: 2021/12/16

ChemScene

Product number: CS-0040187
Product name: RapaLink-1
Purity: ≥98.0%
Packaging: 5mg
Price: $700
Updated: 2021/12/16

ChemScene

Product number: CS-0040187
Product name: RapaLink-1
Purity: ≥98.0%
Packaging: 10mg
Price: $1250
Updated: 2021/12/16

ApexBio Technology

Product number: A8764
Product name: Rapalink-1
Packaging: 25mg
Price: $2000
Updated: 2021/12/16

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RapaLink-1 Chemical Properties,Usage,Production

Uses

RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity[1][2].

in vivo

RapaLink-1 (i.p.; every 5 days for 25 days, then once a week for 11 week) shows potent anti-tumor efficacy^[1].

Animal Model:	BALB/ Cnu/nu mice bearing U87MG intracranial xenografts^[1]
Dosage:	1.5 mg/kg
Administration:	I.p.; every 5 days for 25 days, then once a week for 11 week
Result:	Led to initial regression and subsequent stabilization of tumor size.

IC 50

mTOR

References

[1] Fan Q, et al. A Kinase Inhibitor Targeted to mTORC1 Drives Regression in Glioblastoma. Cancer Cell. 2017 Mar 13;31(3):424-435. DOI:10.1016/j.ccell.2017.01.014
[2] Kuroshima K, et al. Potential new therapy of Rapalink-1, a new generation mammalian target of rapamycin inhibitor, against SU 11248-resistant renal cell carcinoma. Cancer Sci. 2020 May;111(5):1607-1618. DOI:10.1111/cas.14395
[3] Rodrik-Outmezguine VS, et al. Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor. Nature. 2016 Jun 9;534(7606):272-6. DOI:10.1038/nature17963
[4] Mu F, et al. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy both in vivo and vitro. Biochem Biophys Res Commun. 2020 Apr 30;525(2):384-391. DOI:10.1016/j.bbrc.2020.02.084

RapaLink-1 Preparation Products And Raw materials

Raw materials

Preparation Products

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RapaLink-1 Suppliers

China 28 Global 28

ShangHai Caerulum Pharma Discovery Co., Ltd.

Tel: 18149758185
Email: sales-cpd@caerulumpharma.com
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ProdList: 3506
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Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
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Shanghai EFE Biological Technology Co., Ltd.

Tel: 021-65675885 18964387627
Fax: 021-65675885
Email: info@efebio.com
Country: China
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Shanghai Changyan Chem & Tech Co., Ltd.

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Fax: +86 (21) 2024-2659
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ShangHai Biochempartner Co.,Ltd

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Taizhou Crene Biotechnology Co. Ltd.

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HANGZHOU CLAP TECHNOLOGY CO.,LTD

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Country: CHINA
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Hefei fuya biotechnology co. LTD

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Country: China
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Shenzhen Excellent Biotech Co., Ltd.

Tel: 13480692018
Email: ramyan@ex-biotech.com
Country: CHINA
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Absin Bioscience Inc.

Tel: 021-38015121 18438616290
Email: lanwu@univ-bio.com
Country: China
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1887095-82-0, RapaLink-1Related Search:

RapaLink-1

RAPALINK 1;RAPALINK1

Rapamycin, 42-O-[2-[[1-[32-[4-amino-3-(2-amino-5-benzoxazolyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-27-oxo-3,6,9,12,15,18,21,24-octaoxa-28-azadotriacont-1-yl]-1H-1,2,3-triazol-4-yl]methoxy]ethyl]-

N-(4-(4-Amino-3-(2-aminobenzo[d]oxazol-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)butyl)-1-(4-((2-(((1R,2R,4S)-4-((R)-2-((3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-1,5,11,28,29-pentaoxo-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34a-tetracosahydro-3H-23,27-epoxypyrido[2,1-c][1]oxa[4]azacyclohentriacontin-3-yl)propyl)-2-methoxycyclohexyl)oxy)ethoxy)methyl)-1H-1,2,3-triazol-1-yl)-3,6,9,12,15,18,21,24-octaoxa

N-(4-(4-Amino-3-(2-aminobenzo[d]oxazol-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)butyl)-1-(4-((2-(((1R,2R,4S)-4-((R)-2-((3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-1,5,11,28,29-pentaoxo-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34a-tetracosahydro-3H-23,27-epoxypyrido[2,1-c][1]oxa[4]azacyclohentriacontin-3-yl)propyl)-2-methoxycyclohexyl)oxy)ethoxy)methyl)-1H-1,2,3-triazol-1-yl)-3,6,9,12,15,18,21,24-octaoxaheptacosan-27-amide

1887095-82-0

C91H138N12O24

chem-chemical

API