製品番号: HY-101268

CHMFL-ABL-053

CHMFL-ABL-053 (Compound 18a) is a potent, selective, and orally available BCR-ABL, SRC and p38 kinase inhibitor with IC₅₀ values of 70, 90 and 62 nM against ABL1, SRC and p38, respectively.

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CAS 番号: 1808287-83-3
分子式: C₂₈H₂₆F₃N₇O₂
分子量:549.55

保管条件:

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

Data Sheet (266 KB)

CHMFL-ABL-053 構造式

CAS 番号: 1808287-83-3

容量

価格（税別）

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数量

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

p38

62 nM (IC₅₀)

Abl

70 nM (IC₅₀)

SRC

90 nM (IC₅₀)

Bcr-Abl アイソフォーム固有の製品をすべて表示 :

Abl
Bcr-Abl

Src アイソフォーム固有の製品をすべて表示 :

p38 MAPK アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	>10 μM Compound: 18a	Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	>10 μM Compound: 18a	Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.007 μM Compound: 18a	Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.045 μM Compound: 18a	Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.045 μM Compound: 18a	Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.053 μM Compound: 18a	Inhibition of Tel-ABL (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of Tel-ABL (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.073 μM Compound: 18a	Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.14 μM Compound: 18a	Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.2 μM Compound: 18a	Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.313 μM Compound: 18a	Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.363 μM Compound: 18a	Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.44 μM Compound: 18a	Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.6 μM Compound: 18a	Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.98 μM Compound: 18a	Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	1.1 μM Compound: 18a	Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	3.3 μM Compound: 18a	Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	9.25 μM Compound: 18a	Inhibition of BCR/ABL p210-T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
HEL	GI₅₀	>10 μM Compound: 18a	Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
K562	GI₅₀	0.014 μM Compound: 18a	Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
KU812 cell line	GI₅₀	0.025 μM Compound: 18a	Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
MEG-01	GI₅₀	0.016 μM Compound: 18a	Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
MOLM-14	GI₅₀	>10 μM Compound: 18a	Antiproliferative activity against human MOLM14 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human MOLM14 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
MV4-11	GI₅₀	8 μM Compound: 18a	Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
U-937	GI₅₀	>10 μM Compound: 18a	Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]

体外実験

CHMFL-ABL-053 (Compound 18a) inhibits the proliferation of CML cell lines with GI₅₀ of 14, 25 and 16 nM against K562, KU812 and MEG-01, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

CHMFL-ABL-053 (Compound 18a) (50 mg/kg/day) almost completely suppresses tumor progression in the K562 cells inoculated xenograft mouse model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

化学情報

CAS 番号 1808287-83-3
分子量 549.55
分子式 C₂₈H₂₆F₃N₇O₂
SMILES

O=C(C1=CN=C(NC2=CC=C(C)C(N)=C2)N=C1NC)NC3=CC(NC(C4=CC=CC(C(F)(F)F)=C4)=O)=CC=C3C
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 (266 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]. Liang X, et al. Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia. J Med Chem. 2016 Mar 10;59(5):1984-2004. [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)

体積 _(終了) 体積 _(終了)

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.

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CHMFL-ABL-053

Bcr-Abl アイソフォーム固有の製品をすべて表示

Src アイソフォーム固有の製品をすべて表示

p38 MAPK 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

CHMFL-ABL-053 関連分類

HY-101268 関連分類