Ipatasertib
CAS No. : 1001264-89-6
(Synonyms: GDC-0068; RG7440)
| Size | Price | Stock |
|---|---|---|
| 2mg | $60 | In-stock |
| 5mg | $84 | In-stock |
| 10mg | $120 | In-stock |
| 25mg | $245 | In-stock |
| 50mg | $348 | In-stock |
| 100mg | $540 | In-stock |
| 200mg | $900 | In-stock |
| 500mg | $1800 | In-stock |
| 1g | $3120 | In-stock |
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| 10 g | Get quote | |
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| Cat. No. : | HY-15186 |
| M.Wt: | 458.00 |
| Formula: | C24H32ClN5O2 |
| Purity: | >98 % |
| Solubility: | H2O : 3.57 mg/mL (ultrasonic;warming;heat to 60°C);DMSO : 100 mg/mL (ultrasonic) |
Ipatasertib (GDC-0068) 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 synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models[1][2].
IC50 & Target:IC50: 5±7 nM (Akt1), 18±10 nM (Akt2), 8±9 nM (Akt3), 3100±705 nM (PKA)[1]
In Vitro:Ipatasertib (10 µM; 12, 24 h) suppresses colon cancer cell proliferation by p53 irrespectively activating PUMA in vitro[1].
Ipatasertib (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 increases the mRNA level of PUMA in HCT116 WT, p53−/−, and DLD1 (p53 mutant) cells[1].
Ipatasertib (10 µM; 24 h) induces apoptosis through PUMA/Bax pathway in HCT116 cells[1].
In Vivo:Ipatasertib (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].
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