ChemicalBook > CAS DataBase List > KPT-9294

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);KPT-9274 (KPT9274);KPT9274, 10 mM in DMSO;Padnarsertib (KPT-9274);KPT 9274;KPT9274;KPT-9274;(E)-3-(6-aminopyridin-3-yl)-N-((5-(4-(4,4-difluoropiperidine-1-carbonyl)phenyl)-7-(4-fluorophenyl)benzofuran-2-yl)methyl)acrylamide
CBNumber: CB72741566
Molecular Formula: C35H29F3N4O3
Formula Weight: 610.62
MOL File: 1643913-93-2.mol

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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)
color: White to light yellow
InChIKey: MRFOPLWJZULAQD-SWGQDTFXSA-N
SMILES: C(NCC1=CC2=CC(C3=CC=C(C(N4CCC(F)(F)CC4)=O)C=C3)=CC(C3=CC=C(F)C=C3)=C2O1)(=O)/C=C/C1=CC=C(N)N=C1

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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.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 22921
Product name: KPT-9274
Purity: ≥98%
Packaging: 1mg
Price: $49
Updated: 2021/12/16

Cayman Chemical

Product number: 22921
Product name: KPT-9274
Purity: ≥98%
Packaging: 5mg
Price: $221
Updated: 2021/12/16

Cayman Chemical

Product number: 22921
Product name: KPT-9274
Purity: ≥98%
Packaging: 10mg
Price: $392
Updated: 2021/12/16

Cayman Chemical

Product number: 22921
Product name: KPT-9274
Purity: ≥98%
Packaging: 25mg
Price: $858
Updated: 2021/12/16

ApexBio Technology

Product number: B5937
Product name: KPT-9274
Packaging: 50mg
Price: $1300
Updated: 2021/12/16

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KPT-9294 Chemical Properties,Usage,Production

Uses

Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC50s of <100 nM and 120 nM, respectively[1][2][3].

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].

in vivo

Padnarsertib demonstrates a decrement of xenograft growth comparable with that of Sunitinib (HY-10255A). There are minimal Padnarsertib effects on the normal human RPTECs and no apparent toxicity in vivo^[2].
Padnarsertib is currently being investigated in a phase I human clinical trial of patients with advanced solid malignancies and NHL^[2].
Padnarsertib (oral administation; 100mg/kg or 200 mg/kg; twice a day; 14 days) demonstrates a decrement of xenograft growth without no significant weight loss. 8 hours after, Padnarsertib are measured at the end of the experiment in mouse plasma and tumors with 10757 ng/mL and 10647 ng/mL, respectively^[3].

Animal Model:	Mice^[1]
Dosage:	100mg/kg or 200 mg/kg
Administration:	Oral administation; 100mg/kg or 200 mg/kg; twice a day; 14 days
Result:	Showed a significant decrease of xenograft growth in KPT-9274 treated mouse.

IC 50

PAK4: 100 nM (IC₅₀); Nampt: 120 nM (IC₅₀)

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

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KPT-9294 Suppliers

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View Lastest Price from KPT-9294 manufacturers

Zhuozhou Wenxi import and Export Co., Ltd

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

Career Henan Chemical Co

Product: KPT-9294 1643913-93-2
Price: US $1.00/g
Min. Order: 1g
Purity: 99%
Supply Ability: 20kg
Release date: 2019-12-23

1643913-93-2, KPT-9294Related Search:

KPT-9294

PAK4-IN-1

(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)-

Padnarsertib (KPT-9274)

KPT 9274( ATG-019)

(E)-3-(6-aminopyridin-3-yl)-N-((5-(4-(4,4-difluoropiperidine-1-carbonyl)phenyl)-7-(4-fluorophenyl)benzofuran-2-yl)methyl)acrylamide

KPT9274, 10 mM in DMSO

KPT-9274 (KPT9274)

1643913-93-2

C35H29F3N4O3

APIs