SKLB4771 (Synonyms: FLT3-IN-1)

Cat. No.: HY-12960 Purity: 98.08%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

SKLB4771 Chemical Structure

CAS No. : 1370256-78-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 195	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 195	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 500	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
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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.

Molecular Weight

537.66

Formula

C₂₅H₂₇N₇O₃S₂

CAS No.

1370256-78-2

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

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Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
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μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.08%

Select Batch:

Data Sheet (282 KB) SDS (251 KB)

COA (258 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

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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.

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SKLB4771 (Synonyms: FLT3-IN-1)

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SKLB4771 (Synonyms: FLT3-​IN-​1)

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SKLB4771 (Synonyms: FLT3-IN-1)