产品名称

英文名称：Ridaforolimus (Deforolimus, MK-8669)

同义词

Ridaforolimus、Deforolimus、AP23573、MK-8669、572924-54-0、Taltorvic、AP-23573、48Z35KB15K、MK8669、AP 23573、Ridaforolimus, >80%、CHEBI79700、MK 8669、Ridaforolimus [USAN]、RIDAFOROLIMUS [MI]、RIDAFOROLIMUS [INN]、RIDAFOROLIMUS [JAN]、Deforolimus (MK-8669)、Ridaforolimus、AP23573、药雷帕霉素

产品性质

CAS编号：572924-54-0

分子式：C53H84NO14P

分子量：990.21

EC号：682-462-9

PubChem编号：11520894

别名：AP23573|药雷帕霉素

英文别名：Ridaforolimus|Deforolimus|AP23573|MK-8669|572924-54-0|Taltorvic|AP-23573|48Z35KB15K|MK8669|AP 23573|Ridaforolimus, >80%|CHEBI79700|MK 8669|Ridaforolimus [USAN]|RIDAFOROLIMUS [MI]|RIDAFOROLIMUS [INN]|RIDAFOROLIMUS [JAN]|Deforolimus (MK-8669)|Ridaforolimus

规格或纯度：≥95%

英文名称：Ridaforolimus (Deforolimus, MK-8669)

生化机理：Deforolimus is a selective FRAP (mTOR) inhibitor (IC50 of 0.2 nM), used to treat HT-1080 cells induces a dose-dependent inhibition of both S6 and 4E-BP1 phosphorylation, with IC50 of 0.2 nM and 5.6 nM, respectively, and leads to a decrease in cell size, an increase in the proportion of cells in the G1 phase of the cell cycle, and inhibition of glucose uptake. Ridaforolimus shows antiproliferative activity a variety of cell lines with EC50 of 0.2-2.3 nM. Ridaforolimus is a potent and selective inhibitor of VEGF production in a dose-dependent manner. Ridaforolimus treatment causes growth suppression in human NSCLC cell lines with IC30 values of 2.45-8.83 nM, with the exception of H157 with IC30 of >20 nM. Ridaforolimus treatment causes dephosphorylation of p70S6KThr389 in A549, H1703 and H157 cells, except H1666 that may express a resistant variant of mTORC1, and causes increased phosphorylation of pAKTser473 and pAKTThr308 in A549 and H1703 cells.

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：Ridaforolimus (Deforolimus, MK-8669)是一种选择性的mTOR抑制剂，IC50为0.2 nM；对mTOR信号通路的抑制作用及与FKBP12结合能力和Rapamycin接近。A selective FRAP (mTOR) inhibitor

ALogP：5.9

IUPAC Name：(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-12-[(2R)-1-[(1S,3R,4R)-4-dimethylphosphoryloxy-3-methoxycyclohexyl]propan-2-yl]-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone

INCHI：InChI=1S/C53H84NO14P/c1-32-18-14-13-15-19-33(2)44(63-8)30-40-23-21-38(7)53(61,67-40)50(58)51(59)54-25-17-16-20-41(54)52(60)66-45(35(4)28-39-22-24-43(46(29-39)64-9)68-69(11,12)62)31-42(55)34(3)27-37(6)48(57)49(65-10)47(56)36(5)26-32/h13-15,18-19,27,32,34-36,38-41,43-46,48-49,57,61H,16-17,20-26,28-31H2,1-12H3/b15-13+,18-14+,33-19+,37-27+/t32-,34-,35-,36-,38-,39+,40+,41+,43-,44+,45+,46-,48-,49+,53-/m1/s1

InChi Key：BUROJSBIWGDYCN-GAUTUEMISA-N

Canonical SMILES：CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)OP(=O)(C)C)C)C)O)OC)C)C)C)OC

Isomeric SMILES：C[C@@H]1CC[C@H]2C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C[C@H](OC(=O)[C@@H]3CCCCN3C(=O)C(=O)[C@@]1(O2)O)[C@H](C)C[C@@H]4CC[C@H]([C@@H](C4)OC)OP(=O)(C)C)C)/C)O)OC)C)C)/C)OC

关联CAS：572924-54-0

PubChem CID：11520894

MeSH Entry Terms：AP-23573;AP23573;deforolimus;MK 8669;MK-8669;MK8669;ridaforolimus

溶解性：DMSO ≥196mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL

象形图：

信号词：Warning

危险声明：H373 Causes damage to organs through prolonged or repeated exposureH400 Very toxic to aquatic lifeH361 Suspected of damaging fertility or the unborn child

预防措施声明：P273,P280,P405,P501,P260,P391,P203,P318,P319

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