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Ridaforolimus

Ridaforolimus structure

CAS No:
572924-54-0
Formula:
C53H84NO14P
Chemical Name:
Ridaforolimus
Synonyms:
Rapamycin,42-(dimethylphosphinate);AP 23573;Deforolimus;MK 8669;Ridaforolimus;AP 2357;697252-87-2
Categories:
Biochemical Engineering > Inhibitors

Description

Deforolimus (AP23573; MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells.

Ridaforolimus is a small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus binds to and inhibits the mammalian target of rapamycin (mTOR), which may result in cell cycle arrest and, consequently, the inhibition of tumor cell growth and proliferation. Upregulated in some tumors, mTOR is a serine/threonine kinase involved in regulating cellular proliferation, motility, and survival that is located downstream of the PI3K/Akt signaling pathway.

Ridaforolimus Basic Attributes

Molecular Weight：

990.214

Exact Mass：

990.21

UNII：

48Z35KB15K

NCI Thesaurus Code：

C49061

ATC Code：

L - Antineoplastic and immunomodulating agents

Characteristics

PSA：

211.31000

XLogP3：

3.12

Density：

1.2±0.1 g/cm3

Melting Point：

95-98°C

Boiling Point：

996.2±75.0 °C at 760 mmHg

Flash Point：

556.3±37.1 °C

Refractive Index：

1.539

Storage Conditions：

Hygroscopic, -20°C Freezer, Under Inert Atmosphere

Safety Information

GHS Classification：

|Warning|H361 (14.63%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]|P201, P202, P260, P273, P281, P308+P313, P314, P391, P405, and P501|Aggregated GHS information provided by 41 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Investigated for use/treatment in solid tumors, sarcoma, cancer/tumors (unspecified), endometrial cancer, prostate cancer, and bone metastases.

Mechanism of Action：

Deforolimus inhibits the mammalian target of rapamycin (mTOR), a serine kinase of the phosphatidylinositol-3-kinase (PI3K) family that regulates protein synthesis, affecting cell growth and proliferation. mTOR is a downstream effector of the phosphatidylinositol 3-kinase/Akt and nutrient-sensing pathways which cancer cells need to proliferate.

MeSH Entry Terms：

AP-23573

Ridaforolimus Use and Manufacturing

Ridaforolimus is a semisynthetic macrocyclic lactone prepared from rapamycin by selective alkylation of the 42-hydroxy group with a dimethylphosphinate moiety. Like all tacrolimus analogues, ridaforolimus binds to receptor protein, FKBP12. The complex then binds to mTOR preventing its interaction with target proteins. Ridaforolimus is extensively cited in the literature with over 70 citations.

Computed Properties

Molecular Weight:990.2
XLogP3:5.9
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:14
Rotatable Bond Count:8
Exact Mass:989.56294335
Monoisotopic Mass:989.56294335
Topological Polar Surface Area:202
Heavy Atom Count:69
Complexity:1940
Defined Atom Stereocenter Count:15
Defined Bond Stereocenter Count:4
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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