PF-05212384
Gedatolisib (PF-05212384, PKI-587)
CAS: 1197160-78-3
Molecular Formula: C32H41N9O4
PF-05212384 - Names and Identifiers
| Name | Gedatolisib (PF-05212384, PKI-587) |
| Synonyms | CS-46 PKI587 PKI587 PKI-587 PKI 587 GEDATOLISIB PF-05212384 PKI 587 PF 05212384 Gedatolisib (PF-05212384, PKI-587) 1-(4-(4-(dimethylamino)piperidine-1-carbonyl)phenyl)-3-(4-(4,6-dimorpholino-1,3,5-triazin-2-yl)phenyl)urea N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl]urea |
| CAS | 1197160-78-3 |
PF-05212384 - Physico-chemical Properties
| Molecular Formula | C32H41N9O4 |
| Molar Mass | 615.73 |
| Density | 1.364 |
| Melting Point | 226-227°C |
| Solubility | DMSO |
| Appearance | Solid |
| Color | Off-White |
| pKa | 13.97±0.70(Predicted) |
| Storage Condition | Refrigerator |
| Use | Gedatolisib (PF-05212384, PKI-587) is a highly effective, dual PI3Kα, PI3Kγ and mTOR inhibitor with IC50 of 0.4 nM, 5.4 nM and 1.6 nM, respectively. |
| In vitro study | PKI-587 act effectively on the most common mutant forms of PI3Kα, especially H1047R and E545K, with IC50 of 0.6 nM and 0.6 nM, respectively. Consistent with inhibition of PI3K/mTOR signaling pathway protein phosphorylation, PKI-587 inhibited tumor cell growth in MDA-361 and PC3-MM2 cell lines with an IC50 of 4 nM and 13.1 nM, respectively. |
| In vivo study | PKI-587 Intravenous administration to nude mice at a dose of 25 mg/kg resulted in low plasma clearance (7(mL/min)/kg) and high volume distribution (7.2 L/kg), and longer half-life (14.4 hours). PKI-587 produced potent antitumor effects in a MDA-361 xenograft model with a minimum effective dose (MED) of 3 mg/kg and a maximum tolerated dose (MTD) of 30 mg/kg. However, PKI-587 acted on H1975 (non-small cell lung cancer, mutant EGFR [L858R, T790M]) transplanted tumor model at a dose of 25 mg/kg for 7 days. As a result, 90% of the experimental treatment group survived. |
PF-05212384 - Risk and Safety
| HS Code | 29349990 |
PF-05212384 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.624 ml | 8.12 ml | 16.241 ml |
| 5 mM | 0.325 ml | 1.624 ml | 3.248 ml |
| 10 mM | 0.162 ml | 0.812 ml | 1.624 ml |
| 5 mM | 0.032 ml | 0.162 ml | 0.325 ml |
Last Update：2024-01-02 23:10:35
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CAS: 1197160-78-3
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Product Name: Gedatolisib (PF-05212384, PKI-587) Visit Supplier Webpage Request for quotation
CAS: 1197160-78-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1197160-78-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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