CHMFL-ABL/KIT-155 (Synonyms: CHMFL-ABL-KIT-155)

目录号: HY-101034: FAQs
Data Sheet 产品使用指南技术支持

CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) 是一种高效的，具有口服活性的 type II ABL/c-KIT 双激酶抑制剂 (IC₅₀ 分别为 46 nM 和 75 nM)，对 BLK (IC₅₀=81 nM), CSF1R (IC₅₀=227 nM), DDR1 (IC₅₀=116 nM), DDR2 (IC₅₀=325 nM), LCK (IC₅₀=12 nM), PDGFRβ (IC₅₀=80 nM) 激酶也具有明显的抑制活性。CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) 阻止细胞周期进展和诱导细胞凋亡。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CHMFL-ABL/KIT-155 Chemical Structure

CAS No. : 2081093-21-0

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格		是否有货
50 mg		询价
100 mg		询价
250 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

CHMFL-ABL/KIT-155 相关产品

•同靶点产品:

•同靶点蛋白产品:

查看 PDGFR 亚型特异性产品:

查看所有亚型

PDGFR PDGFRβ PDGFRα

查看 Discoidin Domain Receptor 亚型特异性产品:

查看所有亚型

DDR1 DDR2

生物活性
纯度 & 产品资料
参考文献

生物活性

CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC₅₀s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC₅₀=81 nM), CSF1R (IC₅₀=227 nM), DDR1 (IC₅₀=116 nM), DDR2 (IC₅₀=325 nM), LCK (IC₅₀=12 nM) and PDGFRβ (IC₅₀=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis^[1].

IC₅₀ & Target

IC50: 46 nM (type II ABL), 75 nM (c-KIT), 81 nM (BLK), 227 nM (CSF1R), 116 nM (DDR1), 325 nM (DDR2), 12 nM (LCK), 80 nM (PDGFRβ)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	> 10 μM Compound: 34	Growth inhibition of mouse BAF3 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Growth inhibition of mouse BAF3 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	> 10 μM Compound: 34	Inhibition of BCR/ABL p210 fusion protein T315I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of BCR/ABL p210 fusion protein T315I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.012 μM Compound: 34	Inhibition of Tel-fused PDGFR-alpha (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused PDGFR-alpha (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.014 μM Compound: 34	Inhibition of Tel-fused PDGFR-beta (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused PDGFR-beta (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.033 μM Compound: 34	Inhibition of human BCR/ABL p210 fusion protein expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of human BCR/ABL p210 fusion protein expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.035 μM Compound: 34	Inhibition of Tel-fused VEGFR2 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused VEGFR2 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.078 μM Compound: 34	Inhibition of Tel-fused c-KIT V559D mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT V559D mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.124 μM Compound: 34	Inhibition of Tel-fused c-KIT N822K mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT N822K mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.149 μM Compound: 34	Inhibition of Tel-fused c-KIT (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.162 μM Compound: 34	Inhibition of Tel-fused CSF1R (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused CSF1R (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.221 μM Compound: 34	Inhibition of Tel-fused c-KIT L576P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT L576P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.27 μM Compound: 34	Inhibition of BCR/ABL p210 fusion protein M356T mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of BCR/ABL p210 fusion protein M356T mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.386 μM Compound: 34	Inhibition of Tel-fused LCK (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused LCK (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.49 μM Compound: 34	Inhibition of BCR/ABL p210 fusion protein F317I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of BCR/ABL p210 fusion protein F317I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.658 μM Compound: 34	Inhibition of Tel-fused BLK (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused BLK (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.67 μM Compound: 34	Inhibition of BCR/ABL p210 fusion protein F317L mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of BCR/ABL p210 fusion protein F317L mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.98 μM Compound: 34	Inhibition of BCR/ABL p210 fusion protein H369P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of BCR/ABL p210 fusion protein H369P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	1.01 μM Compound: 34	Inhibition of Tel-fused c-KIT T670I/V559D double mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT T670I/V559D double mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	1.67 μM Compound: 34	Inhibition of BCR/ABL p210 fusion protein Y253H mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of BCR/ABL p210 fusion protein Y253H mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	1.84 μM Compound: 34	Inhibition of Tel-fused c-KIT V654A mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT V654A mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	1.85 μM Compound: 34	Inhibition of Tel-fused c-KIT T670I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT T670I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	2.87 μM Compound: 34	Inhibition of Tel-fused c-KIT V559D/V654A double mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT V559D/V654A double mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	5.06 μM Compound: 34	Inhibition of Tel-fused c-KIT D816V mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT D816V mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	6.08 μM Compound: 34	Inhibition of BCR-fused DDR2 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of BCR-fused DDR2 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	9.77 μM Compound: 34	Inhibition of Tel-fused DDR1 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused DDR1 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
CHO	GI₅₀	> 10 μM Compound: 34	Antiproliferative activity against CHO cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against CHO cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
GIST882	GI₅₀	0.095 μM Compound: 34	Antiproliferative activity against human GIST882 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human GIST882 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
GISTT1	GI₅₀	0.023 μM Compound: 34	Antiproliferative activity against human GISTT1 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human GISTT1 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
HL-60	GI₅₀	7.34 μM Compound: 34	Antiproliferative activity against human HL60 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human HL60 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
K562	EC₅₀	< 100 nM Compound: 34	Inhibition of BCR/ABL p210 fusion protein autophosphorylation at Y245 in human K562 cells measured after 2 hrs by immunoblotting Inhibition of BCR/ABL p210 fusion protein autophosphorylation at Y245 in human K562 cells measured after 2 hrs by immunoblotting	[PMID: 27966954]
K562	GI₅₀	0.027 μM Compound: 34	Antiproliferative activity against human K562 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human K562 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
KU812 cell line	GI₅₀	0.056 μM Compound: 34	Antiproliferative activity against human KU812 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human KU812 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
MEG-01	GI₅₀	0.02 μM Compound: 34	Antiproliferative activity against human MEG01 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human MEG01 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
MOLM-14	GI₅₀	8.49 μM Compound: 34	Antiproliferative activity against human MOLM14 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human MOLM14 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
MV4-11	GI₅₀	8.14 μM Compound: 34	Antiproliferative activity against human MV4-11 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human MV4-11 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
Rec1	GI₅₀	3.47 μM Compound: 34	Antiproliferative activity against human Rec1 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human Rec1 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
Sf9	IC₅₀	46 nM Compound: 34	Inhibition of C-terminal His-tagged human ABL1 expressed in baculovirus infected SF9 cells using Tyr 02 peptide as substrate measured after 1 hr by FRET based Z'Lyte assay Inhibition of C-terminal His-tagged human ABL1 expressed in baculovirus infected SF9 cells using Tyr 02 peptide as substrate measured after 1 hr by FRET based Z'Lyte assay	[PMID: 27966954]
U-937	GI₅₀	5.73 μM Compound: 34	Antiproliferative activity against human U937 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human U937 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]

体外研究
(In Vitro)

CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) exhibits anti-proliferation activities in the BCR-ABL dependent CML cancer cell lines such as K562 (GI₅₀: 0.027 µM), MEG-01 (GI₅₀: 0.02 µM), and KU812 (GI₅₀: 0.056 µM). It also potently inhibits the growth of c-KIT dependent GISTs cancer cell lines including GIST-T1 (GI₅₀: 0.023 µM), GIST-882 (GI₅₀: 0.095 µM) but not c-KIT independent GIST-48B (GI₅₀: 3.96 µM) ^[1].

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

体内研究
(In Vivo)

CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) (25-100 mg/kg; p.o.; once daily for 28 days) shows dose-dependent tumor progression suppression without apparent toxicity in female nu/nu mice bearing established K562 tumor xenografts^[1].

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

分子量

609.68

Formula

C₃₃H₃₈F₃N₅O₃

CAS 号

2081093-21-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料

产品使用指南 (1538 KB)

参考文献

[1]. Wang Q, et al. Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Bin [Content Brief]

CHMFL-ABL/KIT-155 相关分类

Cancer

摩尔计算器
稀释计算器

The molarity calculator equation

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

质量		浓度		体积		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)	×	体积 _(start)	=	浓度 _(final)	×	体积 _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CHMFL-ABL/KIT-1552081093-21-0CHMFL-ABL-KIT-155Bcr-Ablc-KitApoptosisPDGFRDiscoidin Domain ReceptorSCFRCD117Platelet-derived growth factor receptorInhibitorinhibitorinhibit

您最近查看的产品:

产品名称：

* 需求量：

* 客户姓名：

* Email：

* 电话：

* 公司或机构名称：

留言给我们：

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。	站点地图隐私声明
沪ICP备15051369号-4 上海工商沪公网安备31011502019417 沪(浦)应急管危经许[2021]201709(QFYS) 营业执照（三证合一）
Copyright © 2013-2025 MedChemExpress. All Rights Reserved.

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

CHMFL-ABL/KIT-155 (Synonyms: CHMFL-ABL-KIT-155)

Customer Review

CHMFL-ABL/KIT-155 相关产品

•同靶点产品:

•同靶点蛋白产品:

查看 PDGFR 亚型特异性产品:

查看 Discoidin Domain Receptor 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

CHMFL-ABL/KIT-155 相关分类

摩尔计算器

稀释计算器

The molarity calculator equation

The dilution calculator equation

Keywords:

您最近查看的产品:

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

产品名称：			* Lot #：
* 客户姓名：			* Email：
电话：			* 部门：
* 公司或机构名称：
留言给我们：

姓名
邮箱 *

Sorry, but the email address you supplied was invalid.

CHMFL-ABL/KIT-155 (Synonyms: CHMFL-ABL-KIT-155)

Customer Review

CHMFL-ABL/KIT-155 相关抗体

CHMFL-ABL/KIT-155 相关产品

•同靶点产品:

•同靶点蛋白产品:

查看 PDGFR 亚型特异性产品:

查看 Discoidin Domain Receptor 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

CHMFL-ABL/KIT-155 相关抗体:

CHMFL-ABL/KIT-155 相关分类

摩尔计算器

稀释计算器

The molarity calculator equation

The dilution calculator equation

Keywords:

您最近查看的产品:

Request for HNMR Report

Request for HNMR Report

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z