| Identification | Back Directory | [Name]
1H-Pyrido[2,3-b][1,4]oxazin-2(3H)-one, 6-[4-(cis-1-amino-3-hydroxycyclobutyl)phenyl]-1-ethyl-7-phenyl- | [CAS]
1313439-71-2 | [Synonyms]
VAD044
ALM301
1H-Pyrido[2,3-b][1,4]oxazin-2(3H)-one, 6-[4-(cis-1-amino-3-hydroxycyclobutyl)phenyl]-1-ethyl-7-phenyl- | [Molecular Formula]
C25H25N3O3 | [MOL File]
1313439-71-2.mol | [Molecular Weight]
415.48 |
| Chemical Properties | Back Directory | [Boiling point ]
664.8±55.0 °C(Predicted) | [density ]
1.278±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
14.69±0.40(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
Engasertib is an orally active highly specific AKT inhibitor with IC50 values of 0.13 μM, 0.09 μM and 2.75 μM for AKT1, AKT2 and AKT3, respectively. Engasertib inhibits AKT phosphorylation and modulates downstream signalling in vitro. Engasertib can inhibit cancer cell proliferation and tumor growth[1]. | [in vivo]
ALM301 (10, 30 and 100 mg/kg; p.o.; single dosage) inhibits pAKTS473 in tumors and suppresses tumor growth[1].
ALM301 (3 or 10 mg/kg; p.o.; q.d. for 49 days) shows better tumor inhibition ability when combined with Tamoxifen.html" class="link-product" target="_blank">Tamoxifen (HY-13757A)[1]. | Animal Model: | BALB/c mice (bearing A549 xenografts)[1] | | Dosage: | 10, 30 and 100 mg/kg | | Administration: | p.o.; single dosage | | Result: | Increased total plasma concentrations dose-dependently that resulted in almost total abrogation of measurable pAKTS473 in tumors at all timepoints over 24 h.
Exhibited the tumour growth inhibition (TGI) of 23, 31 and 41% at 10, 30 and 100 mg/kg, respectively. |
| Animal Model: | BALB/c mice (bearing PIK3CA-mutant MCF-7 xenografts)[1] | | Dosage: | 3 or 10 mg/kg | | Administration: | p.o.; q.d. for 49 days | | Result: | Showed significant tumour regressions of 57% and 50% at 3 and 10 mg/kg, respectively, when combined with Tamoxifen (HY-13757A) (5 mg/kg; q.d.). |
| [IC 50]
AKT1: 0.13 μM (IC50); Akt2: 0.09 μM (IC50); Akt3: 2.75 μM (IC50) | [References]
[1] Page N, et al. Identification and development of a subtype-selective allosteric AKT inhibitor suitable for clinical development. Sci Rep. 2022 Sep 20;12(1):15715. DOI:10.1038/s41598-022-20208-5 |
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BOC Sciences
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1-631-485-4226; 16314854226 |
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https://www.bocsci.com |
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