Capivasertib (AZD5363) effectively inhibited all isoforms of Akt(Akt1/Akt2/3) with an IC50 of 3 nM/8 nM/8 nM in a cell-free assay and had similar inhibitory effects on P70S6K/PKA, with less inhibitory activity against ROC1/2. Phase 2.

 

Brand: BCM

 

Target: Akt; PKA; mTOR; Autophagy

 

Signaling Pathways: Autophagy; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors

In Vitro: Capivasertib inhibited all AKT isoforms with a potency of 10 nmol/L or less and inhibited phosphorylation of AKT substrates in cells with a potency of approximately 0.3 to 0.8 μmol/L. Capivasertib monotherapy inhibited the proliferation of 41 of 182 solid and hematologic tumor cell lines with a potency of 3 μmol/L or less. Cell lines derived from breast cancers showed the highest frequency of sensitivity. There was a significant relationship between the presence of PIK3CA and/or PTEN mutations and sensitivity to Capivasertib and between RAS mutations and resistance.

 

Melting Point: 161-164°C

 

pKa: 13.93±0.50(Predicted)

 

Solubility: Soluble in DMSO; Soluble in Ethanol. Insoluble in Water.

 

GHS: GHS07

 

Isomeric SMILES: C1CN(CCC1(C(=O)N[C@@H](CCO)C2=CC=C(C=C2)Cl)N)C3=NC=NC4=C3C=CN4  

 

InChIKey: JDUBGYFRJFOXQC-KRWDZBQOSA-N  

 

InChI: InChI=1S/C21H25ClN6O2/c22-15-3-1-14(2-4-15)17(6-12-29)27-20(30)21(23)7-10-28(11-8-21)19-16-5-9-24-18(16)25-13-26-19/h1-5,9,13,17,29H,6-8,10-12,23H2,(H,27,30)(H,24,25,26)/t17-/m0/s1

 

Attribute
[Chem Name]	4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide
[Synonym]	Capivasertib; AZD5363
[CAS No.]	1143532-39-1
[MDL No.]	MFCD22628785
[Formula]	C21H25ClN6O2
[Molecular]	428.92
[Form]	Off-White to Pale Beige Solid
[Storage]	Keep in dark place。 Sealed in dry, 2-8°C

Goods Tag

4-[(2-methylpropa...

$90