- KPT-9274
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- $15.00 / 1KG
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2021-07-02
- CAS:1643913-93-2
- Min. Order: 1KG
- Purity: 99%+ HPLC
- Supply Ability: Monthly supply of 1 ton
- KPT-9294
-
- $1.00 / 1g
-
2019-12-24
- CAS:1643913-93-2
- Min. Order: 1g
- Purity: 99%
- Supply Ability: 20kg
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| | KPT-9294 Basic information |
| Product Name: | KPT-9294 | | Synonyms: | KPT-9294;(2E)-3-(6-Amino-3-pyridinyl)-N-[[5-[4-[(4,4-difluoro-1-piperidinyl)carbonyl]phenyl]-7-(4-fluorophenyl)-2-benzofuranyl]methyl]-2-propenamide;CS-1746;KPT 9274;KPT9274;KPT-9274;PAK4-IN-1(KPT9274);2-Propenamide, 3-(6-amino-3-pyridinyl)-N-[[5-[4-[(4,4-difluoro-1-piperidinyl)carbonyl]phenyl]-7-(4-fluorophenyl)-2-benzofuranyl]methyl]-, (2E)-;PAK4-IN-1;Padnarsertib (KPT-9274) | | CAS: | 1643913-93-2 | | MF: | C35H29F3N4O3 | | MW: | 610.62 | | EINECS: | | | Product Categories: | APIs | | Mol File: | 1643913-93-2.mol |  |
| | KPT-9294 Chemical Properties |
| Boiling point | 857.5±65.0 °C(Predicted) | | density | 1.39±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | ≥22.45 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | | form | solid | | pka | 12.96±0.46(Predicted) | | color | White to light yellow |
| | KPT-9294 Usage And Synthesis |
| Biological Activity | kpt-9274 is a selective and orally bioavailable allosteric inhibitor of pak4 [1][2][3].p21 protein (cdc42/rac)-activated kinase 4 (pak4) is a serine/threonine-protein kinase and a member of the pak family of proteins which are rac1 and cdc42 effectors. pak4 is a mediator of filopodia formation and stabilizes β-catenin transcriptional activity, and is involved in disease progression for several solid tumors [1][2][3].kpt-9274 is a selective and orally bioavailable pak4 inhibitor. in mda-mb-468 cells, kpt-9274 showed anti-tumor activity with ic50 value of 0.12 μm. kpt-9274 reduced pak4 protein and the key downstream effectors of cell cycle (β-catenin, cyclin d1), cell migration (cofilin), autophagy (ampk) and apoptosis (caspase and parp cleavage) [1]. in rcc cells, kpt-9274 dose-dependently inhibited cell viability [2]. in aml cell lines, kpt-9274 (1 nm-10 μm) inhibited cell proliferation in a dose-and time- dependent way and reduced protein and mrna expression of pak4 [3].in mice inoculated with mda-mb-231 or mda-mb-468 cells, kpt-9274 were given orally once daily (5 or 7 days/week) without major toxicity. kpt-9274 induced a maximum tgi of ~55% and ~70% in mda-mb-231 and mda-mb-468 mice, respectively [1]. in subcutaneous xenograft mouse models, kpt-9274 inhibited rcc growth [2]. in human aml leukemia xenograft model, kpt-9274 (150 mg/kg) significantly inhibited tumor growth, prevented invasion of mv4-11 cells, and improved overall survival [3]. | | references | [1]. senapedis w, george r, mccauley d, et al. preclinical evaluation of novel pak4 allosteric modulators against triple negative breast cancer.
[2]. aboud oa, senapedis w, landesman y, et al. inhibition of pak4 attenuates renal cell carcinoma (rcc) growth.
[3]. mitchell s, orwick s, cannon m, et al. in vitro and in vivo anti-leukemic effects of kpt-9274, a reported pak4 allosteric modulator, in acute myeloid leukemia: promising results justifying further development in this disease. 57th annual meeting & exposition. orlando, fl december 5-8, 2015. |
| | KPT-9294 Preparation Products And Raw materials |
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