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製品番号: HY-160478

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GNF-6

GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC₅₀s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation.

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CAS 番号: 839708-29-1
分子式: C₂₂H₁₉F₃N₆O₂
分子量:456.42

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (265 KB)

GNF-6 構造式

CAS 番号: 839708-29-1

容量

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

Bcr-Abl アイソフォーム固有の製品をすべて表示 :

Abl
Bcr-Abl

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	2.114 μM Compound: 10k	Growth inhibition of parental mouse BA/F3 cells after 72 hrs by celltiter-glo assay Growth inhibition of parental mouse BA/F3 cells after 72 hrs by celltiter-glo assay	[PMID: 30153003]
BaF3	IC₅₀	<5 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant	[PMID: 20604564]
BaF3	IC₅₀	<5 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant	[PMID: 20604564]
BaF3	IC₅₀	<5 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F317L mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F317L mutant	[PMID: 20604564]
BaF3	IC₅₀	<5 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant	[PMID: 20604564]
BaF3	IC₅₀	<5 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant	[PMID: 20604564]
BaF3	IC₅₀	<5 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant	[PMID: 20604564]
BaF3	IC₅₀	<5 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl	[PMID: 20604564]
BaF3	IC₅₀	1799 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells Antiproliferative activity against mouse BA/F3 cells	[PMID: 20604564]
BaF3	IC₅₀	243 nM Compound: 1, GNF-6	Inhibition of Bcr-Abl T315I mutant autophosphorylation in mouse BA/F3 cells Inhibition of Bcr-Abl T315I mutant autophosphorylation in mouse BA/F3 cells	[PMID: 20604564]
BaF3	IC₅₀	294 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant	[PMID: 20604564]
BaF3	IC₅₀	303 nM Compound: 1, GNF-6	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant	[PMID: 20604564]
OCI-AML-3	GI₅₀	0.466 μM Compound: 10k	Growth inhibition of human OCI-AML3 cells harboring NRAS-Q61L mutant after 72 hrs by celltiter-glo assay Growth inhibition of human OCI-AML3 cells harboring NRAS-Q61L mutant after 72 hrs by celltiter-glo assay	[PMID: 30153003]
U-937	GI₅₀	4.967 μM Compound: 10k	Growth inhibition of parental human U937 cells after 72 hrs by celltiter-glo assay Growth inhibition of parental human U937 cells after 72 hrs by celltiter-glo assay	[PMID: 30153003]

化学情報

CAS 番号 839708-29-1
分子量 456.42
分子式 C₂₂H₁₉F₃N₆O₂
SMILES

O=C(C1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(C)C(N3C(N(C)C4=NC(N)=NC=C4C3)=O)=C2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (265 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. David F. Woodward, et al. Non-acidic cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl derivatives as therapeutic agents. WO1994006433A1. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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生物活性
- 製品説明
化学情報
純度とドキュメンテーション
参考文献

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GNF-6

Bcr-Abl アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

GNF-6 関連分類

HY-160478 関連分類