Comparison

capivasertib

Item no. V4274-50mg
Manufacturer InvivoChem LLC
CASRN 1143532-39-1
Amount 50mg
Category
Type Biochemicals
Specific against other
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Available
Description
InvivoChem Cat #:V4274CAS #:1143532-39-1 Purity >=98%

Description: Capivasertib (formerly known as AZD5363), a novel pyrrolopyrimidine-derived compound, is a potent, orally available pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1, Akt2 and Akt3, respectively. AKT is a key node in the most frequently deregulated signaling network in human cancer. AZD5363 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 umol/L. AZD5363 monotherapy inhibited the proliferation of 41 of 182 solid and hematologic tumor cell lines with a potency of 3 umol/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 AZD5363 and between RAS mutations and resistance. Oral dosing of AZD5363 to nude mice caused dose- and time-dependent reduction of PRAS40, GSK3beta, and S6 phosphorylation in BT474c xenografts (PRAS40 phosphorylation EC(50) ca. 0.1 umol/L total plasma exposure), reversible increases in blood glucose concentrations, and dose-dependent decreases in 218Ffluoro-2-deoxy-D-glucose ((18)F-FDG) uptake in U87-MG xenografts. Chronic oral dosing of AZD5363 caused dose-dependent growth inhibition of xenografts derived from various tumor types, including HER2(+) breast cancer models that are resistant to trastuzumab. AZD5363 also significantly enhanced the antitumor activity of docetaxel, lapatinib, and trastuzumab in breast cancer xenografts. It is concluded that AZD5363 is a potent inhibitor of AKT with pharmacodynamic activity in vivo, has potential to treat a range of solid and hematologic tumors as monotherapy or a combinatorial agent, and has potential for personalized medicine based on the genetic status of PIK3CA, PTEN, and RAS. AZD5363 is currently in phase I clinical trials.

Description:

References: Mol Cancer Ther. 2012 Apr; 11(4):873-87.

References:


Capivasertib

Name: Capivasertib
CAS#: 1143532-39-1
Chemical Formula: C21H25ClN6O2
Exact Mass: 428.17275
Molecular Weight: 428.9152
Elemental Analysis: C, 58.81; H, 5.87; Cl, 8.27; N, 19.59; O, 7.46
Storage
-20C for 3 years in powder form
-80C for 2 years in solvent
Technical Information
Synonym: AZD5363; AZD-5363; AZD 5363
IUPAC/Chemical Name: (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)piperidine-4-carboxamide
InChi Key: JDUBGYFRJFOXQC-KRWDZBQOSA-N
InChi Code: 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
SMILES Code: O=C(C1(N)CCN(C2=C3C(NC=C3)=NC=N2)CC1)N[CH](C4=CC=C(Cl)C=C4)CCO

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 50mg
Available: In stock
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