FT671


Catalog No. Size PriceQuantity
M14803-2 Contact sales@xcessbio.com for quotation $100

Description

FT671 is a potent, non-covalent and selective USP7 inhibitor with an IC50 of 52 nM and binds to the USP7 catalytic domain with a Kd of 65 nM.

Product information

CAS Number: 1959551-26-8

Molecular Weight: 533.48

Formula: C24H23F4N7O3

Chemical Name: 5-({1-[(3S)-4,4-difluoro-3-(3-fluoro-1H-pyrazol-1-yl)butanoyl]-4-hydroxypiperidin-4-yl}methyl)-1-(4-fluorophenyl)-1H,4H,5H-pyrazolo[3,4-d]pyrimidin-4-one

Smiles: OC1(CN2C=NC3=C(C=NN3C3=CC=C(F)C=C3)C2=O)CCN(CC1)C(=O)C[C@@H](C(F)F)N1C=CC(F)=N1

InChiKey: BLSNYSFLZAWBIV-SFHVURJKSA-N

InChi: InChI=1S/C24H23F4N7O3/c25-15-1-3-16(4-2-15)35-22-17(12-30-35)23(37)33(14-29-22)13-24(38)6-9-32(10-7-24)20(36)11-18(21(27)28)34-8-5-19(26)31-34/h1-5,8,12,14,18,21,38H,6-7,9-11,13H2/t18-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 50 mg/mL (93.72 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

FT671 increases p53 protein levels in HCT116 or bone osteosarcoma (U2OS) cell lines, leading to induction of p53 target genes including BBC3 (which encodes PUMA), CDKN1A (p21), RPS27L (S27L) and MDM2. FT671 leads to the degradation of N-Myc and upregulation of p53 in the neuroblastoma cell line IMR-32. FT671 also stabilizes p53 in the MM.1S multiple myeloma cell line, which correlates with increased MDM2 ubiquitination and leads to expression of p53 target genes.

In Vivo:

FT671 (100 mg/kg and 200 mg/kg, Oral gavage, daily) treatment in mice leads to a significant dose-dependent inhibition of tumor growth. And FT671 is well-torelated even at high doses.

Products are for research use only. Not for human use.

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