GNE-272

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406825

CAS#: 1936428-93-1

Description: GNE-272 is a potent and selective in Vivo Probe for the Bromodomains of CBP/EP300 (CBP IC50 = 0.02 μM, EP300 IC50 = 0.03 μM, BRET IC50 = 0.41 μM, BRD4(1) C50 = 13 μM).GNE-272 showed a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model. CBP has also been implicated in neurological disorders where a CBP bromodomain inhibitor has been shown to reduce expression of a regulator of G-protein signaling (RGS4).

Chemical Structure

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GNE-272
CAS# 1936428-93-1
Instruction

Theoretical Analysis

MedKoo Cat#: 406825
Name: GNE-272
CAS#: 1936428-93-1
Chemical Formula: C22H25FN6O2
Exact Mass: 424.20
Molecular Weight: 424.480
Elemental Analysis: C, 62.25; H, 5.94; F, 4.48; N, 19.80; O, 7.54

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: GNE-272; GNE 272; GNE272.

IUPAC/Chemical Name: (S)-1-(3-((2-fluoro-4-(1-methyl-1H-pyrazol-4-yl)phenyl)amino)-1-(tetrahydrofuran-3-yl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethan-1-one

InChi Key: NKOJNOBJGYTLLZ-KRWDZBQOSA-N

InChi Code: InChI=1S/C22H25FN6O2/c1-14(30)28-7-5-21-18(12-28)22(26-29(21)17-6-8-31-13-17)25-20-4-3-15(9-19(20)23)16-10-24-27(2)11-16/h3-4,9-11,17H,5-8,12-13H2,1-2H3,(H,25,26)/t17-/m0/s1

SMILES Code: CC(N1CCC2=C(C(NC3=C(F)C=C(C4=CN(C)N=C4)C=C3)=NN2[C@H]5CCOC5)C1)=O

Appearance: Solid powder

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

Shipping Condition: 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 Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 424.48 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Crawford TD, Romero FA, Lai KW, Tsui V, Taylor AM, de Leon Boenig G, Noland
CL, Murray J, Ly J, Choo EF, Hunsaker TL, Chan EW, Merchant M, Kharbanda S,
Gascoigne KE, Kaufman S, Beresini MH, Liao J, Liu W, Chen KX, Chen Z, Conery AR,
Côté A, Jayaram H, Jiang Y, Kiefer JR, Kleinheinz T, Li Y, Maher J, Pardo E, Poy
F, Spillane KL, Wang F, Wang J, Wei X, Xu Z, Xu Z, Yen I, Zawadzke L, Zhu X,
Bellon S, Cummings R, Cochran AG, Albrecht BK, Magnuson S. Discovery of a Potent
and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J Med
Chem. 2016 Sep 28. [Epub ahead of print] PubMed PMID: 27682507.