Cat. No.: HY-12960

SKLB4771

(Synonyms: FLT3-IN-1)

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SKLB4771 is a potent and selective Flt3 inhibitor with an IC₅₀ value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue.

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Pureté: 99.20%
CAS No.: 1370256-78-2
Formule: C₂₅H₂₇N₇O₃S₂
Masse moléculaire:537.66

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SKLB4771 Chemical Structure

CAS No.: 1370256-78-2

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 10 nM (Flt3); 3.7 μM (Flt4); 1.5 μM (Aurora A); 6.8 μM (c-kit); 2.8 μM (FMS)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	8.91 μM Compound: 20c	Cytotoxicity against human A431 cells after 72 hrs by MTT assay Cytotoxicity against human A431 cells after 72 hrs by MTT assay	[PMID: 22452518]
A549	IC₅₀	>20 μM Compound: 20c	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 22452518]
BT-474	IC₅₀	>20 μM Compound: 20c	Cytotoxicity against human BT474 cells after 72 hrs by MTT assay Cytotoxicity against human BT474 cells after 72 hrs by MTT assay	[PMID: 22452518]
DU-145	IC₅₀	18.6 μM Compound: 20c	Cytotoxicity against human DU145 cells after 72 hrs by MTT assay Cytotoxicity against human DU145 cells after 72 hrs by MTT assay	[PMID: 22452518]
HCC827	IC₅₀	12.5 μM Compound: 20c	Cytotoxicity against human HCC827 cells after 72 hrs by MTT assay Cytotoxicity against human HCC827 cells after 72 hrs by MTT assay	[PMID: 22452518]
HCT-116	IC₅₀	>10 μM Compound: 20c	Cytotoxicity against FLT3-independent human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against FLT3-independent human HCT116 cells after 72 hrs by MTT assay	[PMID: 22452518]
HeLa	IC₅₀	>20 μM Compound: 20c	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 22452518]
Jurkat	IC₅₀	3.05 μM Compound: 20c	Cytotoxicity against human Jurkat cells after 72 hrs by MTT assay Cytotoxicity against human Jurkat cells after 72 hrs by MTT assay	[PMID: 22452518]
K562	IC₅₀	12.65 μM Compound: 20c	Cytotoxicity against human K562 cells after 72 hrs by MTT assay Cytotoxicity against human K562 cells after 72 hrs by MTT assay	[PMID: 22452518]
KARPAS-299	IC₅₀	>20 μM Compound: 20c	Cytotoxicity against human KARPAS299 cells after 72 hrs by MTT assay Cytotoxicity against human KARPAS299 cells after 72 hrs by MTT assay	[PMID: 22452518]
LoVo	IC₅₀	>20 μM Compound: 20c	Cytotoxicity against human LoVo cells after 72 hrs by MTT assay Cytotoxicity against human LoVo cells after 72 hrs by MTT assay	[PMID: 22452518]
MCF7	IC₅₀	>20 μM Compound: 20c	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 22452518]
MDA-MB-231	IC₅₀	>20 μM Compound: 20c	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 22452518]
MV4-11	IC₅₀	0.006 μM Compound: 20c	Cytotoxicity against FLT3-dependent human MV4-11 cells after 72 hrs by MTT assay Cytotoxicity against FLT3-dependent human MV4-11 cells after 72 hrs by MTT assay	[PMID: 22452518]
NCI-H2228	IC₅₀	>20 μM Compound: 20c	Cytotoxicity against human NCI-H2228 cells after 72 hrs by MTT assay Cytotoxicity against human NCI-H2228 cells after 72 hrs by MTT assay	[PMID: 22452518]
NCI-H292	IC₅₀	6.94 μM Compound: 20c	Cytotoxicity against human NCI-H292 cells after 72 hrs by MTT assay Cytotoxicity against human NCI-H292 cells after 72 hrs by MTT assay	[PMID: 22452518]
PC-3	IC₅₀	15.72 μM Compound: 20c	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 22452518]
PC-9	IC₅₀	3.72 μM Compound: 20c	Cytotoxicity against human PC9 cells after 72 hrs by MTT assay Cytotoxicity against human PC9 cells after 72 hrs by MTT assay	[PMID: 22452518]
Ramos	IC₅₀	6.25 μM Compound: 20c	Cytotoxicity against human Ramos cells after 72 hrs by MTT assay Cytotoxicity against human Ramos cells after 72 hrs by MTT assay	[PMID: 22452518]
SH-SY5Y	IC₅₀	>20 μM Compound: 20c	Cytotoxicity against human SH-SY5Y cells after 72 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells after 72 hrs by MTT assay	[PMID: 22452518]
SK-OV-3	IC₅₀	>20 μM Compound: 20c	Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay	[PMID: 22452518]
SW480	IC₅₀	11.16 μM Compound: 20c	Cytotoxicity against human SW480 cells after 72 hrs by MTT assay Cytotoxicity against human SW480 cells after 72 hrs by MTT assay	[PMID: 22452518]
U-937	IC₅₀	>10 μM Compound: 20c	Cytotoxicity against human U937 cells after 72 hrs by MTT assay Cytotoxicity against human U937 cells after 72 hrs by MTT assay	[PMID: 22452518]

In Vitro

SKLB4771 (compound 20c) (72 h) inhibits FLT3-ITD-expressing MV4-11 cells with an IC₅₀ value of 6 nM, and inhibits other cancer cells with IC₅₀s of 3.05 μM (Jurkat), 6.25 μM (Ramos), 3.72 μM (PC-9), 6.94 μM (H292), and 8.91 μM (A431), respectively^[1].
SKLB4771 (0-300 nM; 20 h) inhibits FLT3 phosphorylation and also decreases the phosphorylation of the downstream signaling proteins STAT5 and ERK1/2 at concentrations >0.1 μM^[1].

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

Western Blot Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0, 30, 100, 300 nM
Incubation Time:

20 hours
Result:

Resulted inhibition against the human FLT3 kinase in a dose-dependent manner, and decreased the phosphorylation level of STAT5 and ERK1/2 at 100 nM and 300 nM.

In Vivo

SKLB4771 (20-100 mg/kg; i.p.; once daily; 21 d) inhibits tumor growth in vivo without significant weight loss or any other obvious signs of toxicity on mice^[1].
Pharmacokinetic Analysis of SKLB4771 in rat (40 mg/kg; i.p.)^[1]

C_max (μg/mL)	T_1/2 (h)	AUC_max (h·μg/mL)	T_max (h)	CL_obs (L/h/kg)
5.31	13.9	21.86	1.0	2.21

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

Animal Model:

Female NOD-SCID mouse (6−7 weeks old)^[1]
Dosage:

20, 40, 100 mg/kg; dissolved in 25% (v/v) PEG400 plus 5% DMSO, administered at a dose of 5 mL/kg
Administration:

Intraperitoneal injection; once daily; 21 days
Result:

Inhibited tumor growth by 66% and 84% at concentration of 20 mg/kg and 40 mg/kg, respectively.
Resulted cell proliferation inhibition and apoptosis induction.

Chemical Information

CAS No. 1370256-78-2
Appearance Solid
Masse moléculaire 537.66
Formule C₂₅H₂₇N₇O₃S₂
Color Light yellow to yellow
SMILES

O=C(NC1=NN=C(SC2=C3C=CC(OCCCN4CCOCC4)=CC3=NC=N2)S1)NC5=CC=C(C)C=C5
Synonyms

FLT3-IN-1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

DMSO : 33.33 mg/mL (61.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8599 mL

9.2996 mL

18.5991 mL

5 mM

0.3720 mL

1.8599 mL

3.7198 mL

10 mM

0.1860 mL

0.9300 mL

1.8599 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.65 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Instruction de manipulation (2659 KB)

Références

[1]. Li WW, et al. Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo. J Med Chem. 2012 Apr 26;55(8):3852-66. [Content Brief]

[2]. Yan HX, et al. Accumulation of FLT3(+) CD11c (+) dendritic cells in psoriatic lesions and the anti-psoriatic effect of a selective FLT3 inhibitor. Immunol Res. 2014 Oct;60(1):112-26. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8599 mL	9.2996 mL	18.5991 mL	46.4978 mL
	5 mM	0.3720 mL	1.8599 mL	3.7198 mL	9.2996 mL
	10 mM	0.1860 mL	0.9300 mL	1.8599 mL	4.6498 mL
	15 mM	0.1240 mL	0.6200 mL	1.2399 mL	3.0999 mL
	20 mM	0.0930 mL	0.4650 mL	0.9300 mL	2.3249 mL
	25 mM	0.0744 mL	0.3720 mL	0.7440 mL	1.8599 mL
	30 mM	0.0620 mL	0.3100 mL	0.6200 mL	1.5499 mL
	40 mM	0.0465 mL	0.2325 mL	0.4650 mL	1.1624 mL
	50 mM	0.0372 mL	0.1860 mL	0.3720 mL	0.9300 mL
	60 mM	0.0310 mL	0.1550 mL	0.3100 mL	0.7750 mL

Keywords

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SKLB4771

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

SKLB4771

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

SKLB4771 Related Classifications

HY-12960 Related Classifications