GDC-0980 (RG7422)
GDC-0980 (RG7422)
CAS: 1032754-93-0
Molecular Formula: C23H30N8O3S
GDC-0980 (RG7422) - Names and Identifiers
GDC-0980 (RG7422) - Physico-chemical Properties
| Molecular Formula | C23H30N8O3S |
| Molar Mass | 498.6 |
| Density | 1.399 |
| Melting Point | >202°C (dec.) |
| Solubility | Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Light Yellow |
| pKa | 13.90±0.20(Predicted) |
| Storage Condition | -20°C Freezer |
| In vitro study | GDC-0980 showed potent selective inhibition of class I PI3K and mTOR kinases over most other kinases, with K I of 17 nM for mTOR and PI3Kα,β,δ, and gamma IC50 of 5 nM,27 nM,7 nM, and 14 nM, respectively. In Vitro, GDC-0980 significantly inhibited the cell proliferation of PC3 and MCF7 cells with IC50 of 307 nM and 255 nM, respectively. A recent study showed that GDC-0980 reduces cancer cell activity in prostate cancer (IC50 <200 nM 50%,<500 nM 100%) by inhibiting cell cycle progression and inducing apoptosis, maximum efficacy in breast cancer (IC50 <200 nM 37%,<500 nM 78%) and NSCLC(IC50 <200 nM 29%,<500 nM 88%), potency was low in pancreatic cancer (IC50 <200 nM 13%,<500 nM 67%) and melanoma cell lines (IC50 <200 nM 0%,<500 nM 33%). |
| In vivo study | In PC-3 and MCF-7 neo/HER2 xenograft models, GDC-0980 at a dose of 1 mg/kg exhibited significant antitumor activity by causing tumor growth delay. In addition, the maximum tolerated dose was 7.5 mg/kg GDC-0980 to cause tumor stasis or regression. In mice, intravenous administration of 1 mg/kg GDC-0980 resulted in low clearance (Cl p: 9.2 mL/min/kg,V ss: 1.7 L/kg). At the same time, 80% PEG400 solution at 5 mg/kg, or 50 mg/kg as crystal suspension in 0.5% methylcellulose/0.2% Tween-80 was administered orally, it has good pharmacokinetic parameters. |
GDC-0980 (RG7422) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.006 ml | 10.028 ml | 20.056 ml |
| 5 mM | 0.401 ml | 2.006 ml | 4.011 ml |
| 10 mM | 0.201 ml | 1.003 ml | 2.006 ml |
| 5 mM | 0.04 ml | 0.201 ml | 0.401 ml |
Last Update：2024-01-02 23:10:35
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Product Name: GDC-0980; GNE 390; RG 7422 Visit Supplier Webpage Request for quotationCAS: 1032754-93-0
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CAS: 1032754-93-0
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View History
GDC-0980 (RG7422)
5-氟-3-氮杂双环[3.1.1]庚烷-1-甲酸盐酸盐
GEOGRAPHUTOXIN II (GTXII)
p-Dimethylaminobenzoic acid 2-ethylhexyl ester
TERBUFOS-SULFOXIDE PESTANAL, 100 MG
4-ISO-PROPYLOXYBENZOIC ACID
1ALPHAH,5ALPHAH-莨菪烷-3ALPHA-醇(±)-托品酸酯硫酸盐
CHROMIUM
2-氰基丙烯酸乙二醇单甲醚酯
庚酰草胺 标准品
5-氟-3-氮杂双环[3.1.1]庚烷-1-甲酸盐酸盐
GEOGRAPHUTOXIN II (GTXII)
p-Dimethylaminobenzoic acid 2-ethylhexyl ester
TERBUFOS-SULFOXIDE PESTANAL, 100 MG
4-ISO-PROPYLOXYBENZOIC ACID
1ALPHAH,5ALPHAH-莨菪烷-3ALPHA-醇(±)-托品酸酯硫酸盐
CHROMIUM
2-氰基丙烯酸乙二醇单甲醚酯
庚酰草胺 标准品