CHMFL-FLT3-122

目录号: HY-110293 纯度: 98.47%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

CHMFL-FLT3-122 是一种有效的、选择性的、具有口服活性的 FLT3 激酶，IC₅₀ 为 40 nM。CHMFL-FLT3-122 对 FLT3 的选择性优于 BTK (IC₅₀ 为 421 nM) 和 c-KIT (IC₅₀ 为 559 nM) 激酶。CHMFL-FLT3-122 通过将细胞周期阻滞至 G0/G1 期来诱导细胞凋亡 (apoptosis)。

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CHMFL-FLT3-122 Chemical Structure

CAS No. : 1839150-56-9

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10 mg	￥2940	In-stock
25 mg	￥5320	In-stock
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生物活性
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参考文献

生物活性

CHMFL-FLT3-122 is a potent, selective and orally active FLT3 kinase with an IC₅₀ of 40 nM. CHMFL-FLT3-122 shows selectivity for FLT3 over BTK (IC₅₀ of 421 nM) and c-KIT (IC₅₀ of 559 nM) kinases. CHMFL-FLT3-122 induces apoptosis by arresting the cell cycle into the G0/G1 phase^[1].

IC₅₀ & Target

IC50: 40 nM (FLT3 kinase), 421 nM (BTK), 559 nM (c-KIT)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	0.003 μM Compound: 18; CHMFL-FLT3-122	Inhibition of FLT3 D835V mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of FLT3 D835V mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.004 μM Compound: 18; CHMFL-FLT3-122	Inhibition of FLT3 D835H mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of FLT3 D835H mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.011 μM Compound: 18; CHMFL-FLT3-122	Inhibition of FLT3 ITD mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of FLT3 ITD mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.016 μM Compound: 18; CHMFL-FLT3-122	Inhibition of wild-type FLT3 (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of wild-type FLT3 (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.033 μM Compound: 18; CHMFL-FLT3-122	Inhibition of FLT3 D835Y mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of FLT3 D835Y mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.17 μM Compound: 18; CHMFL-FLT3-122	Inhibition of FLT3-ITD-D835Y mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of FLT3-ITD-D835Y mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.22 μM Compound: 18; CHMFL-FLT3-122	Inhibition of FLT3-ITD-F691L mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of FLT3-ITD-F691L mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.28 μM Compound: 18; CHMFL-FLT3-122	Inhibition of BMX (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of BMX (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.3 μM Compound: 18; CHMFL-FLT3-122	Inhibition of JAK2 (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of JAK2 (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.31 μM Compound: 18; CHMFL-FLT3-122	Inhibition of LCK (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of LCK (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.65 μM Compound: 18; CHMFL-FLT3-122	Inhibition of RET (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of RET (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.68 μM Compound: 18; CHMFL-FLT3-122	Inhibition of PDGFRB (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of PDGFRB (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.88 μM Compound: 18; CHMFL-FLT3-122	Inhibition of HCK (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of HCK (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.94 μM Compound: 18; CHMFL-FLT3-122	Inhibition of BLK (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of BLK (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	1.8 μM Compound: 18; CHMFL-FLT3-122	Inhibition of EGFR (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of EGFR (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	1.9 μM Compound: 18; CHMFL-FLT3-122	Inhibition of c-KIT (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of c-KIT (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	2.2 μM Compound: 18; CHMFL-FLT3-122	Inhibition of MET (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of MET (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	2.5 μM Compound: 18; CHMFL-FLT3-122	Inhibition of JAK3 (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of JAK3 (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	3.8 μM Compound: 18; CHMFL-FLT3-122	Inhibition of JAK1 (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of JAK1 (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	4.9 μM Compound: 18; CHMFL-FLT3-122	Cytotoxicity against mouse BAF3 cells assessed as cell proliferation after 72 hrs by CelltiterGlo assay Cytotoxicity against mouse BAF3 cells assessed as cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
JVM-2	GI₅₀	2.6 μM Compound: 18; CHMFL-FLT3-122	Antiproliferative activity against human JVM2 cells after 72 hrs by CelltiterGlo assay Antiproliferative activity against human JVM2 cells after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
MOLM-13	EC₅₀	< 30 nM Compound: 18; CHMFL-FLT3-122	Inhibition of FLT3 mediated Stat5 phosphorylation in human MOLM13 cells for 4 hrs by immunoblot analysis Inhibition of FLT3 mediated Stat5 phosphorylation in human MOLM13 cells for 4 hrs by immunoblot analysis	[PMID: 26630553]
MOLM-13	GI₅₀	0.021 μM Compound: 18; CHMFL-FLT3-122	Antiproliferative activity against human MOLM13 cells after 72 hrs by CelltiterGlo assay Antiproliferative activity against human MOLM13 cells after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
MOLM-13	EC₅₀	100 nM Compound: 18; CHMFL-FLT3-122	Inhibition of FLT3 autophosphorylation at Tyr589/591 residue in human MOLM13 cells for 4 hrs by immunoblot analysis Inhibition of FLT3 autophosphorylation at Tyr589/591 residue in human MOLM13 cells for 4 hrs by immunoblot analysis	[PMID: 26630553]
MOLM-13	GI₅₀	21 nM Compound: CHMFL-FLT3-122	Growth inhibition of human MOLM-13 cells incubated for 72 hrs by CCK-8 assay Growth inhibition of human MOLM-13 cells incubated for 72 hrs by CCK-8 assay	[PMID: 32659083]
MOLM-14	EC₅₀	< 30 nM Compound: 18; CHMFL-FLT3-122	Inhibition of FLT3 autophosphorylation at Tyr589/591 residue in human MOLM14 cells for 4 hrs by immunoblot analysis Inhibition of FLT3 autophosphorylation at Tyr589/591 residue in human MOLM14 cells for 4 hrs by immunoblot analysis	[PMID: 26630553]
MOLM-14	EC₅₀	< 30 nM Compound: 18; CHMFL-FLT3-122	Inhibition of FLT3 mediated Stat5 phosphorylation in human MOLM14 cells for 4 hrs by immunoblot analysis Inhibition of FLT3 mediated Stat5 phosphorylation in human MOLM14 cells for 4 hrs by immunoblot analysis	[PMID: 26630553]
MOLM-14	GI₅₀	0.042 μM Compound: 18; CHMFL-FLT3-122	Antiproliferative activity against human MOLM14 cells after 72 hrs by CelltiterGlo assay Antiproliferative activity against human MOLM14 cells after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
MOLM-14	GI₅₀	42 nM Compound: CHMFL-FLT3-122	Growth inhibition of human MOLM-14 cells incubated for 72 hrs by CCK-8 assay Growth inhibition of human MOLM-14 cells incubated for 72 hrs by CCK-8 assay	[PMID: 32659083]
MV4-11	EC₅₀	< 30 nM Compound: 18; CHMFL-FLT3-122	Inhibition of FLT3 autophosphorylation at Tyr589/591 residue in human MV4-11 cells for 4 hrs by immunoblot analysis Inhibition of FLT3 autophosphorylation at Tyr589/591 residue in human MV4-11 cells for 4 hrs by immunoblot analysis	[PMID: 26630553]
MV4-11	EC₅₀	< 30 nM Compound: 18; CHMFL-FLT3-122	Inhibition of FLT3 mediated Stat5 phosphorylation in human MV4-11 cells for 4 hrs by immunoblot analysis Inhibition of FLT3 mediated Stat5 phosphorylation in human MV4-11 cells for 4 hrs by immunoblot analysis	[PMID: 26630553]
MV4-11	GI₅₀	0.022 μM Compound: 18; CHMFL-FLT3-122	Antiproliferative activity against human MV4-11 cells after 72 hrs by CelltiterGlo assay Antiproliferative activity against human MV4-11 cells after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
MV4-11	GI₅₀	22 nM Compound: CHMFL-FLT3-122	Growth inhibition of human MV4-11 cells incubated for 72 hrs by CCK-8 assay Growth inhibition of human MV4-11 cells incubated for 72 hrs by CCK-8 assay	[PMID: 32659083]
NAMALVA	GI₅₀	6.4 μM Compound: 18; CHMFL-FLT3-122	Antiproliferative activity against human NAMALWA cells after 72 hrs by CelltiterGlo assay Antiproliferative activity against human NAMALWA cells after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
NB-4	GI₅₀	3.8 μM Compound: 18; CHMFL-FLT3-122	Antiproliferative activity against human NB4 cells after 72 hrs by CelltiterGlo assay Antiproliferative activity against human NB4 cells after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
SU-DHL-2	GI₅₀	5.5 μM Compound: 18; CHMFL-FLT3-122	Antiproliferative activity against human SU-DHL-2 cells after 72 hrs by CelltiterGlo assay Antiproliferative activity against human SU-DHL-2 cells after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
U2932	GI₅₀	1.6 μM Compound: 18; CHMFL-FLT3-122	Antiproliferative activity against human U2932 cells after 72 hrs by CelltiterGlo assay Antiproliferative activity against human U2932 cells after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
U-937	GI₅₀	9.7 μM Compound: 18; CHMFL-FLT3-122	Antiproliferative activity against human U937 cells after 72 hrs by CelltiterGlo assay Antiproliferative activity against human U937 cells after 72 hrs by CelltiterGlo assay	[PMID: 26630553]

体外研究
(In Vitro)

CHMFL-FLT3-122（化合物18）显着抑制FLT3-ITD阳性急性髓性白血病（AML）癌细胞系MV4-11（GI₅₀ = 22 nM）、MOLM13/14（GI₅₀ = 21 nM/42 nM）的增殖^[1]。
CHMFL-FLT3-122（0.03-1 μM；24 小时）可以阻止这些细胞系的细胞周期进展至 G0/G1 期并诱导细胞凋亡^[1]。
CHMFL-FLT3-122 (0.03-1 μM; 24 h) 显着抑制 FLT3 Tyr589/591 位点的自磷酸化，并抑制 Stat5 ERK、AKT 的磷酸化和 cMYC^[1] .

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

Cell Cycle Analysis^[1]

Cell Line:	MV4-11, MOML14 and MOLM13 cells
Concentration:	0.03 μM, 0.1 μM, 0.3 μM, 1 μM
Incubation Time:	24 h
Result:	Arrested cell cycle progression.

Western Blot Analysis^[1]

Cell Line:	MV4-11, MOML14 and MOLM13 cells
Concentration:	0.03 μM, 0.1 μM, 0.3 μM, 1 μM
Incubation Time:	24 h
Result:	Significantly affected FLT3 auto-phosphorylation at Tyr589/591 site.

体内研究
(In Vivo)

CHMFL-FLT3-122（12.5-50 mg/kg；口服灌胃；每天一次；持续 22 天）几乎可以完全抑制肿瘤进展，并且不显着影响小鼠体重^[1]。

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

Animal Model:	Female nu/nu mice injected with MV4-11cells^[1]
Dosage:	12.5 mg/kg, 25 mg/kg and 50 mg/kg
Administration:	Oral gavage; once a day; for 22 days
Result:	Could almost completely suppress the tumor progression.

分子量

471.55

Formula

C₂₆H₂₉N₇O₂

CAS 号

1839150-56-9

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 125 mg/mL (265.08 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1207 mL	10.6033 mL	21.2067 mL
5 mM	0.4241 mL	2.1207 mL	4.2413 mL
10 mM	0.2121 mL	1.0603 mL	2.1207 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

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

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)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

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纯度 & 产品资料

纯度: 98.47%

选择批次：

Data Sheet (617 KB) SDS (251 KB)

COA (290 KB) HNMR (296 KB) LCMS (96 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Xixiang Li, et al. Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia. J Med Chem. 2015 Dec 24;58(24):9625-38. [Content Brief]

CHMFL-FLT3-122 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1207 mL	10.6033 mL	21.2067 mL	53.0166 mL
	5 mM	0.4241 mL	2.1207 mL	4.2413 mL	10.6033 mL
	10 mM	0.2121 mL	1.0603 mL	2.1207 mL	5.3017 mL
	15 mM	0.1414 mL	0.7069 mL	1.4138 mL	3.5344 mL
	20 mM	0.1060 mL	0.5302 mL	1.0603 mL	2.6508 mL
	25 mM	0.0848 mL	0.4241 mL	0.8483 mL	2.1207 mL
	30 mM	0.0707 mL	0.3534 mL	0.7069 mL	1.7672 mL
	40 mM	0.0530 mL	0.2651 mL	0.5302 mL	1.3254 mL
	50 mM	0.0424 mL	0.2121 mL	0.4241 mL	1.0603 mL
	60 mM	0.0353 mL	0.1767 mL	0.3534 mL	0.8836 mL
	80 mM	0.0265 mL	0.1325 mL	0.2651 mL	0.6627 mL
	100 mM	0.0212 mL	0.1060 mL	0.2121 mL	0.5302 mL

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-FLT3-1221839150-56-9FLT3ApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3FLT3 Inhibitorarrest cell cycleG0/G1 phaseInhibitorinhibitorinhibit

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CHMFL-FLT3-122

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