WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205836
CAS#: 1222104-37-1
Description: DS-7423 is an orally bioavailable inhibitor of phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinase in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. PI3K/mTOR kinase inhibitor DS-7423 inhibits both PI3K kinase and mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in susceptible tumor cells. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K. Consequently, this agent may potentially be more potent than an agent that inhibits either PI3K kinase or mTOR kinase.
MedKoo Cat#: 205836
Name: DS-7423
CAS#: 1222104-37-1
Chemical Formula: C22H27F3N10O2
Exact Mass: 520.2271
Molecular Weight: 520.5212
Elemental Analysis: C, 50.76; H, 5.23; F, 10.95; N, 26.91; O, 6.15
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Synonym: DS7423; DS 7423; DS-7423;
IUPAC/Chemical Name: (R)-1-(4-(2-(2-aminopyrimidin-5-yl)-6-morpholino-9-(2,2,2-trifluoroethyl)-9H-purin-8-yl)-2-methylpiperazin-1-yl)ethan-1-one
InChi Key: SOJJMSYMCLIQCZ-CYBMUJFWSA-N
InChi Code: InChI=1S/C22H27F3N10O2/c1-13-11-33(3-4-34(13)14(2)36)21-29-16-18(32-5-7-37-8-6-32)30-17(15-9-27-20(26)28-10-15)31-19(16)35(21)12-22(23,24)25/h9-10,13H,3-8,11-12H2,1-2H3,(H2,26,27,28)/t13-/m1/s1
SMILES Code: CC(N1[C@H](C)CN(C2=NC3=C(N4CCOCC4)N=C(C5=CN=C(N)N=C5)N=C3N2CC(F)(F)F)CC1)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 520.5212 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Makii C, Ikeda Y, Oda K, Uehara Y, Nishijima A, Koso T, Kawata Y, Kashiyama T, Miyasaka A, Sone K, Tanikawa M, Tsuruga T, Mori-Uchino M, Nagasaka K, Matsumoto Y, Wada-Hiraike O, Kawana K, Hasegawa K, Fujiwara K, Aburatani H, Osuga Y, Fujii T. Anti-tumor activity of dual inhibition of phosphatidylinositol 3-kinase and MDM2 against clear cell ovarian carcinoma. Gynecol Oncol. 2019 Nov;155(2):331-339. doi: 10.1016/j.ygyno.2019.08.028. Epub 2019 Sep 5. PMID: 31493899.
2: Yokota T, Bendell J, LoRusso P, Tsushima T, Desai V, Kenmotsu H, Watanabe J, Ono A, Murugesan B, Silva J, Naito T, Greenberg J, Kumar P, Wang Y, Jikoh T, Shiga R, Hyman DM, Ho AL, Spriggs DR, Schwartz GK, Gounder MM. Impact of race on dose selection of molecular-targeted agents in early-phase oncology trials. Br J Cancer. 2018 Jun;118(12):1571-1579. doi: 10.1038/s41416-018-0102-1. Epub 2018 May 24. PMID: 29795308; PMCID: PMC6008299.
3: Oda K, Ikeda Y, Kashiyama T, Miyasaka A, Inaba K, Fukuda T, Asada K, Sone K, Wada-Hiraike O, Kawana K, Osuga Y, Fujii T. Characterization of TP53 and PI3K signaling pathways as molecular targets in gynecologic malignancies. J Obstet Gynaecol Res. 2016 Jul;42(7):757-62. doi: 10.1111/jog.13018. Epub 2016 Apr 20. PMID: 27094348.
4: Kashiyama T, Oda K, Ikeda Y, Shiose Y, Hirota Y, Inaba K, Makii C, Kurikawa R, Miyasaka A, Koso T, Fukuda T, Tanikawa M, Shoji K, Sone K, Arimoto T, Wada- Hiraike O, Kawana K, Nakagawa S, Matsuda K, McCormick F, Aburatani H, Yano T, Osuga Y, Fujii T. Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220. doi: 10.1371/journal.pone.0087220. PMID: 24504419; PMCID: PMC3913610.
