Avitinib
Avitinib
CAS: 1557267-42-1
Molecular Formula: C26H26FN7O2
Avitinib - Names and Identifiers
Avitinib - Physico-chemical Properties
| Molecular Formula | C26H26FN7O2 |
| Molar Mass | 487.53 |
| Density | 1.365±0.06 g/cm3(Predicted) |
| pKa | 12.48±0.50(Predicted) |
| Storage Condition | 2-8 ℃, dark |
| MDL | N/A |
| In vitro study | AC0010 selectively inhibits the activated EGFR and EGFR(T790M) mutants with over 298-fold greater potency than the wild type. In NCI-H1975 and NIH/3T3_TC32T8 cells, AC0010 selectively inhibited the phosphorylation of mutant EGFR with IC50 of 7.3 nM and 2.8 nM, respectively, this was about 115 and 298 times more sensitive than AC0010 to inhibit wild-type EGFR phosphorylation in A431 cells. In NCI-H1975 cells, AC0010 potently inhibited EGFR-Tyr1068 phosphorylation with a 65-fold selectivity ratio in NCI-H1975 and A431 cells. In addition to inhibiting EGFR-Tyr1068 phosphorylation, AC0010 also inhibits phosphorylation of downstream targets Akt and ERK1/2. In the detection selectivity experiment, AC0010 at a concentration of 1 μm has more than 80% inhibitory effect on 33 kinases (349 kinases to be tested), including JAK3, BTK and TEC family members. However, the potency of AC0010 inhibition of these kinases in cell experiments is much lower than in enzyme activity experiments. In the relevant cell experiments for BTK and JAK3, The IC50 was 59 nM and 360 nM, respectively. In another library containing 55 molecular targets (receptors, ion channels, transporters), AC0010 at a concentration of 1 μm inhibits the binding of radioligand to 5 targets with an inhibitory effect of more than 50%, including Adenosine A3, L-type calcium channel (Cav1.2), dopamine transporter, 5-HT2A and 5-HT2B. Then in cell function experiments, AC0010 had no inhibitory effect on these five targets. |
| In vivo study | Oral administration of AC0010(500 mg/kg/day) for more than 143 days resulted in complete regression of tumours with activating EGFR and T90M mutations in a xenograft model. In the pharmacokinetic study, in the NCI-H1975 xenograft model, intravenous injection of 10 mg/kg AC0010, the overall clearance and distribution capacity were 5.91 L/h/kg and 14.76 L/kg, respectively, with a terminal half-life of about 1.73 hours, indicating that AC0010 can be rapidly distributed to various tissues, including tumor tissues. After oral administration of 12.5 mg/kg, 50 mg/kg and 200 mg/kg(1 day or 8 consecutive days), the appearance time of the highest concentration of AC0010 in plasma is about 1-2 hours after administration, oral bioavailability is 15.9-41.1%. In animal models, the off-target effects and skin damage of AC0010 and its metabolites have not been found yet. In patients with EGFR T790m(+) NSCLC, Avitinib was well tolerated and effective, with low concentrations in cerebrospinal fluid and weak blood-brain barrier penetration, but good control of brain metastases. |
Avitinib - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.051 ml | 10.256 ml | 20.512 ml |
| 5 mM | 0.41 ml | 2.051 ml | 4.102 ml |
| 10 mM | 0.205 ml | 1.026 ml | 2.051 ml |
| 5 mM | 0.041 ml | 0.205 ml | 0.41 ml |
Last Update：2024-01-02 23:10:35
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CAS: 1557267-42-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Spot supply
Product Name: Abivertinib; AC0010 Visit Supplier Webpage Request for quotationCAS: 1557267-42-1
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: Avitinib Visit Supplier Webpage Request for quotationCAS: 1557267-42-1
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: Avitinib (AC0010) Visit Supplier Webpage Request for quotationCAS: 1557267-42-1
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Product Name: Avitinib Visit Supplier Webpage Request for quotation
CAS: 1557267-42-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 1557267-42-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
View History
Avitinib
103300-74-9
58498-11-6
200628-33-7
1009826-93-0
4-bromo-3-nitropyridine
119532-26-2
18677-41-3
1169770-52-8
Fumonisin
103300-74-9
58498-11-6
200628-33-7
1009826-93-0
4-bromo-3-nitropyridine
119532-26-2
18677-41-3
1169770-52-8
Fumonisin