Ipatasertib tosylate (Synonyms: GDC-0068 tosylate; RG7440 tosylate)

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Ipatasertib (GDC-0068) tosylate is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC₅₀ values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models.

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

Ipatasertib tosylate Chemical Structure

CAS No. : 1491138-24-9

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Other In-stock Forms of Ipatasertib tosylate:

Ipatasertib Ipatasertib dihydrochloride

Other Forms of Ipatasertib tosylate:

39 Publications Citing Use of MCE Ipatasertib tosylate

: Ipatasertib tosylate purchased from MedChemExpress. Usage Cited in: Front Oncol. 2021 Nov 24:11:766298. [Abstract]; Ipatasertib (0.625, 1.25, 5 µM; 24 h) increases the phosphorylation of AKT in MFM-223 FGFR2amp cells.

: Ipatasertib tosylate purchased from MedChemExpress. Usage Cited in: Skelet Muscle. 2021 Mar 15;11(1):6. [Abstract]; The western blot analysis and quantification of phosphorylated and all forms of AKT and P70, MyoG, and MyoD, after transfecting miR-1290/miR-NC with or without GDC0068. GDC-0068 inhibits miR-1290-activated phosphorylation of AKT and P70 in C2C12 myoblasts.

: Ipatasertib tosylate purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2020 Oct;180:114145. [Abstract]; C2C12 myoblasts were pre-incubated with 2.5 μM GDC-0068 for 30 min then treated with 0.2 μM S-Rg3. After incubation with S-Rg3 for 72 h and 24 h, Western blotting is used to detect levels of Myf5 and myogenin in C2C12 myoblasts after incubation of cells with S-Rg3 for 120 h. GDC-0068 inhibits S-Rg3-activated phosphorylation of Akt and mTOR in C2C12 myoblasts.

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Description

IC₅₀ & Target

Akt1

5 nM (IC₅₀)

Akt2

18 nM (IC₅₀)

Akt3

8 nM (IC₅₀)

PKA

3100 nM (IC₅₀)

In Vitro

Ipatasertib tosylate (10 µM; 12, 24 h) suppresses colon cancer cell proliferation by p53 irrespectively activating PUMA in vitro^[1].
Ipatasertib tosylate (1, 5, 10, 20 μM; 24 h/10 μM; 3, 6, 12, 24 h) up-regulates the expression level of PUMA in a concentration and time dependent manner in HCT116 cells^[1].
Ipatasertib tosylate increases the mRNA level of PUMA in HCT116 WT, p53^−/−, and DLD1 (p53 mutant) cells^[1].
Ipatasertib tosylate (10 µM; 24 h) induces apoptosis through PUMA/Bax pathway in HCT116 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:	HCT116 WT, p53^−/−, and DLD1 (p53 mutant) cells
Concentration:	10 µM
Incubation Time:	12, 24 h
Result:	Decreased all the three cell lines viability.

Apoptosis Analysis^[1]

Cell Line:	HCT116 cells
Concentration:	10 µM
Incubation Time:	24 h
Result:	Induced apoptosis through PUMA/Bax pathway.

Western Blot Analysis^[1]

Cell Line:	HCT116 WT, p53^−/−, and DLD1 (p53 mutant) cells
Concentration:	1, 5, 10, 20 μM for 24 h/10 μM for 3, 6, 12, 24 h
Incubation Time:	24 h; 3, 6, 12, 24 h
Result:	Increased the level of PUMA in a concentration and time dependent manner.

In Vivo

Ipatasertib tosylate (30 mg/kg; p.o.; single daily for 15 consecutive days) exhibits PUMA-dependent antitumor activity in HCT116 WT and PUMA^−/− cells xenograft nude mice model^[1].

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

Animal Model:	HCT116 WT and PUMA^−/− cells xenograft nude mice model^[1].
Dosage:	30 mg/kg
Administration:	Oral gavage; single daily for 15 consecutive days.
Result:	Inhibited growth of tumors in a PUMA-dependent manner.

Molecular Weight

630.20

Formula

C₃₁H₄₀ClN₅O₅S

CAS No.

1491138-24-9

SMILES

O=S(O)(C1=CC=C(C=C1)C)=O.ClC2=CC=C([C@@H](CNC(C)C)C(N3CCN(C4=C([C@H](C)C[C@H]5O)C5=NC=N4)CC3)=O)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Sun L, et al. Ipatasertib, a novel Akt inhibitor, induces transcription factor FoxO3a and NF-κB directly regulates PUMA-dependent apoptosis. Cell Death Dis. 2018 Sep 5;9(9):911. [Content Brief]

Ipatasertib tosylate Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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