KPT-9294
- Product Name
- 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
- Formula Weight
- 610.62
- MOL File
- 1643913-93-2.mol
KPT-9294 Property
- 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)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 22921
- Product name
- KPT-9274
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $49
- Updated
- 2021/12/16
- Product number
- 22921
- Product name
- KPT-9274
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $221
- Updated
- 2021/12/16
- Product number
- 22921
- Product name
- KPT-9274
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $392
- Updated
- 2021/12/16
- Product number
- 22921
- Product name
- KPT-9274
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $858
- Updated
- 2021/12/16
- Product number
- B5937
- Product name
- KPT-9274
- Packaging
- 50mg
- Price
- $1300
- Updated
- 2021/12/16
KPT-9294 Chemical Properties,Usage,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
KPT-9294 Suppliers
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View Lastest Price from KPT-9294 manufacturers
- Product
- KPT-9274 1643913-93-2
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-06-26
- Product
- KPT-9294 1643913-93-2
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 20kg
- Release date
- 2019-12-23