KPT-9294
- CAS No.
- 1643913-93-2
- Chemical Name:
- KPT-9294
- Synonyms
- PAK4-IN-1;CS-1746;KPT-9294;PAK4-IN-1(KPT9274);KPT 9274( ATG-019);Padnarsertib (KPT-9274);KPT 9274;KPT9274;KPT-9274;(2E)-3-(6-Amino-3-pyridinyl)-N-[[5-[4-[(4,4-difluoro-1-piperidinyl)carbonyl]phenyl]-7-(4-fluorophenyl)-2-benzofuranyl]methyl]-2-propenamide;2-Propenamide, 3-(6-amino-3-pyridinyl)-N-[[5-[4-[(4,4-difluoro-1-piperidinyl)carbonyl]phenyl]-7-(4-fluorophenyl)-2-benzofuranyl]methyl]-, (2E)-
- CBNumber:
- CB72741566
- Molecular Formula:
- C35H29F3N4O3
- Molecular Weight:
- 610.62
- MDL Number:
- MFCD30207881
- MOL File:
- 1643913-93-2.mol
| 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) |
| FDA UNII | 9T56TV18X7 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
KPT-9294 price More Price(12)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 22921 | KPT-9274 ≥98% | 1643913-93-2 | 1mg | $49 | 2021-12-16 | Buy |
| Cayman Chemical | 22921 | KPT-9274 ≥98% | 1643913-93-2 | 5mg | $221 | 2021-12-16 | Buy |
| Cayman Chemical | 22921 | KPT-9274 ≥98% | 1643913-93-2 | 10mg | $392 | 2021-12-16 | Buy |
| Cayman Chemical | 22921 | KPT-9274 ≥98% | 1643913-93-2 | 25mg | $858 | 2021-12-16 | Buy |
| ApexBio Technology | B5937 | KPT-9274 | 1643913-93-2 | 50mg | $1300 | 2021-12-16 | Buy |
KPT-9294 Chemical Properties,Uses,Production
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
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24738 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Chemtour Biotech Co., Ltd | +8617327281506 | market@chemtour.com | China | 1471 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
