| Company Name: |
Shanghai Yifei Biotechnology Co. , Ltd.
|
| Tel: |
021-65675885 18964387627 |
| Email: |
customer_service@efebio.com |
| Products Intro: |
Product Name:FD223
CAS:2050524-24-6
Purity:95.00% Package:2mg;5mg;25mg
|
| Company Name: |
TargetMol Chemicals Inc.
|
| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:FD223
CAS:2050524-24-6
Package:2mg/RMB 1540;5mg/RMB 2610;25mg/RMB 9160
|
Benzenesulfonamide, N-[2-chloro-5-(1H-pyrazolo[3,4-b]pyridin-5-yl)-3-pyridinyl]- manufacturers
- FD223
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- $916.00 / 25mg
-
2024-10-28
- CAS:2050524-24-6
- Min. Order:
- Purity:
- Supply Ability: 10g
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| | Benzenesulfonamide, N-[2-chloro-5-(1H-pyrazolo[3,4-b]pyridin-5-yl)-3-pyridinyl]- Basic information |
| | Benzenesulfonamide, N-[2-chloro-5-(1H-pyrazolo[3,4-b]pyridin-5-yl)-3-pyridinyl]- Chemical Properties |
| Boiling point | 652.7±65.0 °C(Predicted) | | density | 1.556±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 100 mg/mL (259.18 mM; Need ultrasonic) | | pka | 6.54±0.40(Predicted) | | form | Solid | | color | Off-white to brown |
| | Benzenesulfonamide, N-[2-chloro-5-(1H-pyrazolo[3,4-b]pyridin-5-yl)-3-pyridinyl]- Usage And Synthesis |
| Biological Activity | FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML[1].
FD223 exhibits notable anti-proliferative activities in the p110δ-positive AML cell lines HL-60, MOLM-16, EOL-1 and KG-1, with the IC50 of 2.25 μM, 0.87 μM, 2.82 μM, and 5.82 μM, respectively. FD223 shows weak anti-proliferative activity against p110δ unexpressed MM.1R cell line, with the IC50 value of 23.13 μM[1].FD223 (MOLM-16 cells; 0.1-5 μM; 16 hours) dose-dependently reduces phosphorylation of Akt (Ser473), which is consistent with the positive control Idelalisib, illustrating that the activity of PI3K/Akt pathway in MOLM-16 cell is blocked[1].FD223 (MOLM-16 cells; 24 hours; 1-5 μM) arrests the cell cycle at the G1 phase similar to that of positive control Idelalisib[1].FD223 (1-5 μM; 48 hours) dose-dependently induces cellular apoptosis[1].
FD223 (20 and 40 mg/kg; p.o, per day for 14 consecutive days) displays potent antitumor efficacy in MOLM-16 xenograft model with the tumor volume reduction of 49% at a dose of 40 mg/kg/day (po), and shows no significant toxicity in the preliminary safety assessment[1].FD223 (i.v.; dose of 2 mg/kg; p.o.; 10 mg/kg rats) shows a moderate plasma clearance rate after intravenous administration with C =0.191 L?h-1?kg-1. In the po route, it shows a half-life (t1/2) of 3.74 h and a Cmax of 1104 ng/mL, good oral plasma exposures (AUC0-∞>9000 h?ng/mL) and acceptable oral bioavailability (17.6%)[1]. | | References | [1]. Yang C, et al. Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation [published online ahead of print, 2021 Jun 21]. Eur J Med Chem. 2021;223:113661. |
| | Benzenesulfonamide, N-[2-chloro-5-(1H-pyrazolo[3,4-b]pyridin-5-yl)-3-pyridinyl]- Preparation Products And Raw materials |
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