AZD5363
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- ₹0
- Product name: AZD5363
- CAS: 1143532-39-1
- MF: C21H25ClN6O2
- MW: 428.92
- EINECS:
- MDL Number:MFCD22628785
- Synonyms:AZD5356;AZD5363;4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide;4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide AZD5363;AZD 5363 dihydrochloride;AZD5363;AZD-5363;AZD 5363;(S)-4-Amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidi;AZD5363, 99%, a potent pan-AKT kinase inhibitor
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Properties
Melting point :161-164°C
Density :1.381
storage temp. :Refrigerator
solubility :DMSO (Slightly), Methanol (Slightly)
pka :13.93±0.50(Predicted)
form :Solid
color :Off-White to Pale Beige
Density :1.381
storage temp. :Refrigerator
solubility :DMSO (Slightly), Methanol (Slightly)
pka :13.93±0.50(Predicted)
form :Solid
color :Off-White to Pale Beige
Safety Information
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Description
Akt functions as a key component in multiple signaling pathways including those related to cell proliferation, metabolism, and survival as well as angiogenesis. AZD 5363 is a pyrrolopyrimidine-derived compound that inhibits Akt by competitively binding to the kinase domain, preventing substrate phosphorylation by Akt. It inhibits Akt1, 2, and 3 with IC50 values of 3, 7, and 7 nM, respectively and also inhibits P70S6K and PKA with similar potency (IC50s = 6 and 7 nM, respectively). Furthermore, AZD 5363 shows >75% inhibition at 1 μM against ROCK-II, MKK1, MSK1, MSK2, PKCγ, PKGα, PKGβ, PRKX, RSK2, and RSK3. At 3 μM or less, AZD 5363 has been reported to inhibit the proliferation of 41 out of 182 solid and hematologic tumor cell lines, demonstrating the greatest sensitivity towards breast cancer derived-cells or those with PIK3CA and/or PTEN mutations. Oral dosing to nude mice bearing BT474c xenografts resulted in antitumor activity, including the reduction of the phosphorylation of PRAS40, GSK3β, and S6 at an EC50 value of ~ 0.1 μM.More related product prices
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