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[CAS NO. 1001264-89-6]  Ipatasertib

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PRODUCTS SPECIFICATIONS [1001264-89-6]

Catalog
HY-15186
Brand
MCE
CAS
1001264-89-6

DESCRIPTION [1001264-89-6]

Overview

MDLMFCD22124514
Molecular Weight458.00
Molecular FormulaC24H32ClN5O2
SMILESClC1=CC=C([C@@H](CNC(C)C)C(N2CCN(C3=C([C@H](C)C[C@H]4O)C4=NC=N3)CC2)=O)C=C1

For research use only. We do not sell to patients.

26 Publications Citing Use of MCE


Summary

Ipatasertib (GDC-0068) is a highly selective and ATP-competitive pan-Akt inhibitor with IC 50 s of 5, 18 and 8 nM for Akt1 , Akt2 and Akt3 , respectively.


IC50 & Target

Akt1

5 nM (IC 50 )

Akt3

8 nM (IC 50 )

Akt2

18 nM (IC 50 )

PKA

3100 nM (IC 50 )


In Vitro

Ipatasertib (GDC-0068) shows more than 600 and more than 100-fold selectivity for Akt1 in IC 50 against the closely related kinases PKA and p70S6K, respectively. When tested at 1 μM in a panel of 230 protein kinases, which includes 36 human AGC family members, GDC-0068 inhibits only 3 other kinases by more than 70% at 1 μM concentration (PRKG1α, PRKG1β, and p70S6K). IC 50 s measured for these 3 kinases are 98, 69, and 860 nM, respectively. Thus, with the exception of PKG1 (relative to which Ipatasertib (GDC-0068) is >10-fold more selective for Akt1), Ipatasertib (GDC-0068) displays a more than 100-fold selectivity for Akt1 over the next most potently inhibited non-Akt kinase, p70S6K, in the screening kinase panel. The relationship between pharmacokinetics (PK) and pharmacodynamics (PD) of Ipatasertib (GDC-0068) is investigated in 3 xenograft models that showed dose-dependent response to drug treatment: MCF7-neo/HER2, TOV-21G.x1, and LNCaP. The mean cell viability IC 50 of GDC-0068 in these 3 cell lines is 2.56, 0.44, and 0.11 μM, respectively [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


In Vivo

Ipatasertib (GDC-0068) is typically efficacious in xenograft models in which Akt is activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplifications, or HER2 overexpression. In these models, tumor growth delay, stasis, or regression is achieved at or below 100 mg/kg daily oral dose, which is the maximum dose tested in immunocompromised mice that is well tolerated. When tested in vivo, daily dosing of Ipatasertib (GDC-0068) in combination with RP-56976 induces tumor regression and stasis in the PC-3 and MCF7-neo/HER2 xenograft models, at doses where each single agent is ineffective or only causes modest tumor growth delay. Similarly, increased TGI is observed in the OVCAR3 ovarian cancer xenograft model when Ipatasertib (GDC-0068) is combined with NSC 241240. The combination of Ipatasertib (GDC-0068) with RP-56976 or NSC 241240 is tolerated with less than 5% body weight loss when compared with treatment with each chemotherapeutic agent alone [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT04650581 Canadian Cancer Trials Group|Hoffmann-La Roche
Breast Cancer
December 1, 2020 Phase 3
NCT04467801 Jun Zhang, MD, PhD|University of Iowa|University of Kentucky|University of Kansas Medical Center
NSCLC Stage IV|NSCLC Stage IIIB
September 14, 2021 Phase 2
NCT01485861 Genentech, Inc.
Prostate Cancer
January 11, 2012 Phase 1|Phase 2

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 220 mg/mL ( 480.35 mM ; Need ultrasonic)

H 2 O : 3.57 mg/mL ( 7.79 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1834 mL 10.9170 mL 21.8341 mL
5 mM 0.4367 mL 2.1834 mL 4.3668 mL
10 mM 0.2183 mL 1.0917 mL 2.1834 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 0.5% MC >> 0.5% Tween-80

    Solubility: 10 mg/mL (21.83 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

  • 4.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

1-Propanone, 2-(4-chlorophenyl)-1-[4-[(5R,7R)-6,7-dihydro-7-hydroxy-5-methyl-5H-cyclopentapyrimidin-4-yl]-1-piperazinyl]-3-[(1-methylethyl)amino]-, (2S)-
(2S)-2-(4-Chlorophenyl)-1-[4-[(5R,7R)-6,7-dihydro-7-hydroxy-5-methyl-5H-cyclopentapyrimidin-4-yl]-1-piperazinyl]-3-[(1-methylethyl)amino]-1-propanone
GDC 0068
Ipatasertib
RG 7440
RG7440
RG-7440

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