A rapamycin analog that selectively inhibits mTOR in mTORC1
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MK-8669

Item No. 10543

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
42-(dimethylphosphinate)rapamycin
CAS Number
572924-54-0
Synonyms
  • AP23573
  • Deforolimus
  • Ridaforolimus
Molecular Formula
C53H84NO14P
Formula Weight
990.2
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS(pH7.2) (1:2): 0.33 mg/mlDMSO: 20 mg/mlEthanol: 5 mg/ml
λmax
204, 267, 277, 289 nm
SMILES
O=C(C(N1[C@@](C(O[C@@]([C@H](C)C[C@H]2C[C@@H](OC)[C@H](OP(C)(C)=O)CC2)([H])CC([C@H](C)/C=C(C)/[C@@H](O)[C@H](C([C@H](C)C[C@H](C)/C=C/C=C/C=C(C)/[C@@H](OC)C3)=O)OC)=O)=O)([H])CCCC1)=O)[C@]4(O)O[C@@]3([H])CC[C@H]4C
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    MK-8669 is a rapamycin analog that selectively inhibits mTOR (IC50 = 0.2 nM). Like rapamycin, MK-8669 binds FKBP12 to form a complex that associates with the FKBP-rapamycin binding domain on mTOR and allosterically inhibits mTORC1 kinase activity.1 MK-8669 is more water soluble than rapamycin and is amenable to oral or intravenous administration. Formulations containing rapalogs, including MK-8669, have promise against a subset of cancers, including advanced kidney cancer.1 MK-8669 is also being examined for effectiveness against cancers when used in combination with other chemotherapeutic compounds.2,3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Benjamin, D., Colombi, M., Moroni, C., et al. Rapamycin passes the torch: A new generation of mTOR inhibitors. Nat. Rev. Drug Discov. 10(11), 868-880 (2011).

    2. Becker, M.A., Hou, X., Tienchaianada, P., et al. Ridaforolimus (MK-8669) synergizes with dalotuzumab (MK-0646) in hormone-sensitive breast cancer. BMC Cancer 16(1), 814 (2016).

    3. Hernandez, S.F., Chisholm, S., Borger, D., et al. Ridaforolimus improves the anti-tumor activity of dual HER2 blockade in uterine serous carcinoma in vivo models with HER2 gene amplification and PIK3CA mutation. Gynecol. Oncol. 141(3), 570-579 (2016).

    4. Lamhamedi-Cherradi, S.-E., Menegaz, B.A., Ramamoorthy, V., et al. IGF-1R and mTOR blockade: Novel resistance mechanisms and synergistic drug combinations for Ewing sarcoma. J. Natl. Cancer Inst. 108(12), (2016).

    Product Citations

    Baumgartner, L., Sosa, S., Atanasov, A.G., et al. Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. J. Nat. Prod. 74(8), 1779-1786 (2011).