KPT-9274 free base · Synonyms: Padnarsertib

Padnarsertib is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase inhibitor.

For research use only. Not for human or veterinary use.

Target PAK NAMPT

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

KPT-9274 structure

CAS No.: 1643913-93-2

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 780.00	BP-02125-100mg	In stock	Get quote
250 mg	USD 1,400.00	BP-02125-250mg	In stock	Get quote
500 mg	USD 2,150.00	BP-02125-500mg	In stock	Get quote
1 g	USD 3,500.00	BP-02125-1g	In stock	Get quote

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Description

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

Biological activity

In Vitro Padnarsertib attenuates the PAK4/β-catenin pathway, results in NAD depletion, and attenuates viability, invasion, and migration in several RCC cell lines. Inhibition of NAMPT in a cell-free enzymatic assay using recombinant NAMPT shows an IC50 of approximately 120 nM for Padnarsertib. Padnarsertib attenuates G2–M transit and induces apoptosis in RCC cell lines. 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. Padnarsertib is currently being investigated in a phase I human clinical trial of patients with advanced solid malignancies and NHL. 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.

Identifiers

SMILES: NC1=CC=C(\C=C\C(=O)NCC2=CC3=CC(=CC(=C3O2)C2=CC=C(F)C=C2)C2=CC=C(C=C2)C(=O)N2CCC(F)(F)CC2)C=N1
InChIKey: MRFOPLWJZULAQD-SWGQDTFXSA-N

Specifications

MW (average): 610.6250
Formula: C₃₅H₂₉F₃N₄O₃
CAS No.: 1643913-93-2
Physical state: Solid
Color: white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. WO2015003166A1

[2]. Abu Aboud O, et al. Dual and Specific Inhibition of NAMPT and PAK4 By KPT-9274 Decreases Kidney Cancer Growth. Mol Cancer Ther. 2016 Sep;15(9):2119-29.

[3]. Abu Aboud O, et al. Dual and Specific Inhibition of NAMPT and PAK4 By KPT-9274 Decreases Kidney Cancer Growth.Mol Cancer Ther. 2016 Sep;15(9):2119-29.

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