RapaLink-1

Background

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

More

Less

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

More

Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

More

Less

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

More

Less

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

Background

RapaLink-1 is a small-molecule inhibitor of the mammalian target of rapamycin, a Ser/Thr protein kinase that functions as an ATP and amino acid sensor to balance nutrient availability and cell growth. mTOR inhibitors, such as rapamycin, are used to inhibit the PIK3K-AKT-mTOR pathway, which is a commonly activated pathway in human cancers. RapaLink-1 is an example of a third-generation mTOR inhibitor, which combines the effects of both first-generation and second-generation mTOR inhibitors. Specifically, RapaLink-1 combines the high specificity binding and inhibition of mTORC1 found in rapamycin with the broader specificity of the second-generation mTOR inhibitors, which inhibit both mTORC1 and mTORC2. Several studies have demonstrated that RapaLink-1 can display therapeutic effects in glioblastoma, follicular lymphoma, and renal cell carcinoma, often overcoming resistance to earlier-generation mTOR inhibitors.

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

More

Less

RapaLink-1 Suppliers

China 31 Global 31

ShangHai Caerulum Pharma Discovery Co., Ltd.

Tel: 18149758185 18149758185
Email: sales-cpd@caerulumpharma.com
Country: China
ProdList: 3505
Advantage: 58

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4817
Advantage: 55

Shanghai EFE Biological Technology Co., Ltd.

Tel: 021-65675885 18964387627
Fax: 021-65675885
Email: info@efebio.com
Country: China
ProdList: 9803
Advantage: 58

Shanghai Changyan Chem & Tech Co., Ltd.

Tel: 18930833303 18930833303
Fax: +86 (21) 2024-2659
Email: sales@changyanchem.cn
Country: China
ProdList: 5001
Advantage: 55

ShangHai Biochempartner Co.,Ltd

Tel: 177-54423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 8000
Advantage: 62

Shandong utilizing biological technology co., LTD

Tel: 15966937598
Fax: 3407640895 3071519937
Email: 3407650895@qq.com
Country: China
ProdList: 4111
Advantage: 58

Taizhou Crene Biotechnology Co. Ltd.

Tel: +86-0576-88813233 +86-13396860566
Email: sales@pharm-intermediates.com
Country: China
ProdList: 1982
Advantage: 58

HANGZHOU CLAP TECHNOLOGY CO.,LTD

Tel: 86-571-88216897,88216896 13588875226
Fax: 86-571-88216895
Email: sales@hzclap.com
Country: CHINA
ProdList: 6312
Advantage: 58

Hefei fuya biotechnology co. LTD

Tel: 18096409024
Email: sales02@foreversyn.com
Country: China
ProdList: 1923
Advantage: 58

Shenzhen Excellent Biotech Co., Ltd.

Tel: 13480692018
Email: ramyan@ex-biotech.com
Country: CHINA
ProdList: 954
Advantage: 58

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