CHMFL-FLT3-122

Name: CHMFL-FLT3-122
Brand: MedChemExpress
SKU: HY-110293
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製品番号: HY-110293 純度: 98.47%: Data Sheet SDS COA 取扱説明書
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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.

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CHMFL-FLT3-122 構造式

CAS 番号 : 1839150-56-9

容量	価格（税別）	在庫状況	数量
5 mg	$280	在庫あり	Estimated Time of Arrival: December 31
10 mg	$420	在庫あり	Estimated Time of Arrival: December 31
25 mg	$710	在庫あり	Estimated Time of Arrival: December 31
50 mg	$995	在庫あり	Estimated Time of Arrival: December 31
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製品説明

IC₅₀ & Target

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

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	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	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	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]
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]
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]

体外実験

CHMFL-FLT3-122 (compound 18) significantly inhibits the proliferation of FLT3-ITD positive acute myeloid leukemia (AML) cancer cell lines MV4-11 (GI₅₀ = 22 nM), MOLM13/14 (GI₅₀ = 21 nM/42 nM)^[1].
CHMFL-FLT3-122 (0.03-1 μM; 24 h) could arrest cell cycle progression of these cell lines into the G0/G1 phase and induction of apoptosis^[1].
CHMFL-FLT3-122 (0.03-1 μM; 24 h) significantly inhibits FLT3 auto-phosphorylation at Tyr589/591 site, and also inhibits the phosphorylation of Stat5 ERK, AKT and expression of cMYC^[1].

MedChemExpress (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.

体内実験

CHMFL-FLT3-122 (12.5-50 mg/kg; oral gavage; once a day; for 22 days) could almost completely suppress the tumor progression, and does not significantly affect the mice body weight^[1].

MedChemExpress (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

分子式

C₂₆H₂₉N₇O₂

CAS 番号

1839150-56-9

Appearance

Solid

Color

White to off-white

SMILES

NC1=C2C(N([C@H]3CN(CCC3)C(CN(C)C)=O)N=C2C4=CC=C(OC5=CC=CC=C5)C=C4)=NC=N1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

DMSO : 125 mg/mL (265.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

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純度とドキュメンテーション

純度: 98.47%

Select Batch:

データシート (277 KB) SDS (251 KB)

COA (253 KB) HNMR (296 KB) LCMS (96 KB)

取扱説明書 (2659 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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

CHMFL-FLT3-122 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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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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CHMFL-FLT3-122 関連抗体

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Complete Stock Solution Preparation Table

CHMFL-FLT3-122 Related Classifications

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