RG 7440
GDC-0068
CAS: 1001264-89-6
Molecular Formula: C24H32ClN5O2
RG 7440 - Names and Identifiers
RG 7440 - Physico-chemical Properties
| Molecular Formula | C24H32ClN5O2 |
| Molar Mass | 458 |
| Density | 1.254 |
| Melting Point | >106°C (dec.) |
| Boling Point | 669.4±55.0 °C(Predicted) |
| Solubility | Soluble in DMSO. |
| Appearance | Solid |
| Color | Peach |
| pKa | 13.11±0.40(Predicted) |
| Storage Condition | Hygroscopic, Refrigerator, under inert atmosphere |
| In vitro study | On a large panel of 230 kinases tested, GDC-0068 inhibited only 3 kinases, more than 70% at a concentration of 1 μm, (inhibition of PRKG1α,PRKG1β, and p70S6K, the IC50 was 98 nM, 69 nM, and 860 nM, respectively). GDC-0068 the selectivity of Akt was more than 100 times higher than that of PKA, and the IC50 of Akt was 3.1 μm. GDC-0068 treatment of LNCaP, PC3 and BT474M1 cells inhibited phosphorylation of Akt substrate PRAS40 with an IC50 of 157 nM, 197 nM, and 208 nM, respectively. Moreover, GDC-0068 selectively inhibited cell cycle progression and Akt signaling driven cancer cell viability, including tumor suppressor PTEN deficiency, PIK3CA oncogene mutation, and HER2 amplification, the effect was strongest in the HER2 + and Luminal subtypes. [1-4] |
| In vivo study | GDC-0068 orally treated PC3 prostate xenograft model induced p-PRAS40 down-regulation. GDC-0068 treatment of BT474-Tr xenografts reduced pS6 and peIF4G levels, repositioned FOXO3a to the nucleus, and induced feedback upregulation of HER3 and pERK. GDC-0068 treatment of multiple xenograft models with potent anticancer activity, including PTEN-deficient prostate cancer models LNCaP and PC3, PIK3CA H1047R mutant breast cancer model KPL-4, and MCF7-neo/HER2 tumor model. [1-4] |
RG 7440 - Reference
| Reference Show more | Note: part of our products can only provide part of the information, our company does not guarantee the authority of the information provided, only for the customer reference Exchange research. configuration solution concentration reference: 1mg5mg10mg1mm2.183 ml10.917 ml21.834 ml5mm0.437 ml2.183 ml4.367 ml10mm0.218 ml1.092 ml2.183 50mm0.044ml0.437ml storage conditions:-20C Product Description |
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