{5-[2,4-Bis-(3-methyl-morpholin-4-yl)-pyrido[2,3-d]pyrimidin-7-yl]-2-methoxy-phenyl}-methanol
AZD-8055
CAS: 1009298-09-2
Molecular Formula: C25H31N5O4
{5-[2,4-Bis-(3-methyl-morpholin-4-yl)-pyrido[2,3-d]pyrimidin-7-yl]-2-methoxy-phenyl}-methanol - Names and Identifiers
{5-[2,4-Bis-(3-methyl-morpholin-4-yl)-pyrido[2,3-d]pyrimidin-7-yl]-2-methoxy-phenyl}-methanol - Physico-chemical Properties
| Molecular Formula | C25H31N5O4 |
| Molar Mass | 465.54 |
| Density | 1.248 |
| Melting Point | 204 - 207°C |
| Boling Point | 694.3±65.0 °C(Predicted) |
| Water Solubility | Soluble in DMSO (up to 30 mg/ml) |
| Solubility | Soluble in DMSO (up to 30 mg/ml) |
| Appearance | Form Yellow powder. Color Yellow |
| Color | Yellow |
| pKa | 14.20±0.10(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| Use | AZD8055 is a new type of ATP competitive mTOR inhibitor. IC50 in MDA-MB-468 cells is 0.8 nM. Compared with PI3K subtype and ATM/DNA-PK, it has excellent selectivity (about 1000 times). AZD8055 can induce caspase-dependent apoptosis and autophagy. |
| In vitro study | AZD8055 showed low activity against all PI3K subtypes (α, β, γ, δ) and other near-PI3K kinase families (ATM and DNA-PK). AZD8055 inhibits the phosphorylation of mTORC1(p70S6K and 4E-BP1) ,mTORC2 (AKT) and downstream proteins. AZD8055 completely inhibited the T37/46 phosphorylation site of 4E-BP1 against Rapamycin, resulting in significant inhibition of cap-dependent translation. AZD8055 effectively inhibited U87MG, A549 and H838 cell proliferation with IC50 of 53, 50, and 20 nM, respectively. AZD8055 also induced autophagy and increased LC3-II levels in H838 and A549 cells. AZD8055 reduces leukemia cell proliferation and cell cycle progression, reduces clonal growth of leukemia progenitor cells, and induces caspase-dependent apoptosis in leukemia cells, however, this induction does not occur in normal immature CD34 cells. AZD8055 inhibits the pediatric preclinical testing plan (PPTP) cell line with an IC50 of 24.7 μm and induces a clear distinction in the EFS profile. |
| In vivo study | AZD8055 inhibited pS6 and pAKT in U87MG and A549 xenografts at a dose of 2.5/10 mg/kg, resulting in inhibition of tumor growth. AZD8055 showed significant anticancer activity when treated with 10/20 mg/kg dose of various transplanted tumors including U87MG, BT474c, A549, Calu-3, LoVo, SW620, PC3 and MES-SA. AZD8055 induced a reduction in tumor volume of approximately 40%, accompanied by excision of AKT, S6K, and SGK protein kinase phosphorylation. Treatment of PTEN +/− LKB1 +/hypo xenografts with AZD8055 (5 mg/kg twice daily) and SAHA (100 mg/kg/day) resulted in total inhibition of tumor growth, and there was no side effect on murine mTORC1 and mTORC2 signal inhibition. |
{5-[2,4-Bis-(3-methyl-morpholin-4-yl)-pyrido[2,3-d]pyrimidin-7-yl]-2-methoxy-phenyl}-methanol - Risk and Safety
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| HS Code | 29335990 |
{5-[2,4-Bis-(3-methyl-morpholin-4-yl)-pyrido[2,3-d]pyrimidin-7-yl]-2-methoxy-phenyl}-methanol - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.148 ml | 10.74 ml | 21.48 ml |
| 5 mM | 0.43 ml | 2.148 ml | 4.296 ml |
| 10 mM | 0.215 ml | 1.074 ml | 2.148 ml |
| 5 mM | 0.043 ml | 0.215 ml | 0.43 ml |
Last Update：2024-01-02 23:10:35
{5-[2,4-Bis-(3-methyl-morpholin-4-yl)-pyrido[2,3-d]pyrimidin-7-yl]-2-methoxy-phenyl}-methanol - Target
| Target | Value |
| mTOR (truncated) (MDA-MB-468 cells) |
0.13 nM |
| mTOR (full length) (MDA-MB-468 cells) |
0.8 nM |
Last Update：2024-04-09 01:59:50
{5-[2,4-Bis-(3-methyl-morpholin-4-yl)-pyrido[2,3-d]pyrimidin-7-yl]-2-methoxy-phenyl}-methanol - In vitro study
AZD8055 action on all PI3K subtypes (α, β, & gamma;, & delta;) and other near PI3K kinase families (ATM and DNA-PK) showed low activity. AZD8055 inhibited the phosphorylation of mTORC1(p70S6K and 4E-BP1) ,mTORC2 (AKT) and downstream proteins. AZD8055 completely inhibited the T37/46 phosphorylation site of 4E-BP1 anti-Rapamycin, resulting in obvious inhibition of cap-dependent translation. AZD8055 effectively inhibited U87MG, A549 and H838 cell proliferation with IC50 of 53, 50 and 20 nM respectively. AZD8055 acts on H838 and A549 cells, also induces autophagy and increases LC3-II levels. AZD8055 reduce the proliferation and cell cycle progression of leukemia cells, reduce the clone growth of leukemia progenitor cells, and induce caspase-dependent apoptosis in leukemia cells, but this induction will not occur when acting on normal immature CD34 cells. AZD8055 inhibition of pediatric preclinical test plan (PPTP) cell line, IC50 is 24.7 nM, and the induction of EFS distribution is significantly different.
Last Update：2024-04-09 20:52:54
{5-[2,4-Bis-(3-methyl-morpholin-4-yl)-pyrido[2,3-d]pyrimidin-7-yl]-2-methoxy-phenyl}-methanol - In vivo studies
AZD8055 acts on U87MG and A549 transplanted tumors at a dose of 2.5/10 mg/kg to inhibit pS6 and pAKT, resulting in tumor growth inhibition. When AZD8055 treated a variety of transplanted tumors including U87MG, BT474c, A549, Calu-3, LoVo, SW620, PC3 and MES-SA at a dose of 10/20 mg/kg, it showed obvious anticancer activity. AZD8055 induced tumor volume drop of about 40%, accompanied by resection of AKT, S6K, and SGK protein kinase phosphorylation. PTEN +/& minus was treated with AZD8055 (5 mg/kg twice a day) and SAHA (100 mg/kg/day); LKB1 +/hypo transplanted tumor resulted in total inhibition of tumor growth and no side effects on mTORC1 and mTORC2 signal inhibition in mice.
Last Update：2024-04-09 20:52:54
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Product Name: (5-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol Visit Supplier Webpage Request for quotationCAS: 1009298-09-2
Tel: 18301782025
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Spot supply
Product Name: (5-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol Visit Supplier Webpage Request for quotationCAS: 1009298-09-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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