PLX647

Cat. No.: HY-13838 Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PLX647 is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC₅₀s of 28 and 16 nM, respectively. PLX647 shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC₅₀s=91 and 130 nM, respectively).

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

PLX647 Chemical Structure

CAS No. : 873786-09-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Other Forms of PLX647:

PLX647 dihydrochloride Get quote

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Biological Activity
Purity & Documentation
References
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Description

In Vitro

In vitro, PLX647 potently inhibits proliferation of BCR-FMS cells, with an IC₅₀ of 92 nM. A corresponding Ba/F3 cell line expressing BCR-KIT is also quite sensitive to PLX647, with an IC₅₀ of 180 nM. PLX647 also inhibits endogenous FMS and KIT, as demonstrated by inhibition of the ligand-dependent cell lines M-NFS-60 (IC₅₀=380 nM) and M-07e (IC₅₀=230 nM), which express FMS and KIT, respectively^[1].
PLX647 potently inhibits the growth of FLT3–ITD-expressing MV4-11 cells (IC₅₀=110 nM). PLX647 displayed minimal inhibition of the proliferation of Ba/F3 cells expressing BCR–KDR (IC₅₀=5 μM). PLX647 inhibits osteoclast differentiation with an IC₅₀ of 0.17 μM^[1].

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

In Vivo

PLX647 (40 mg/kg; p.o.; twice daily for 7 days) reduces macrophage accumulation in UUO kidney and blood monocytes^[1].
PLX647 (40 mg/kg; p.o.; male Swiss Webster mice) reduces LPS-induced TNF-α and IL-6 release^[1].
PLX647 (20-80 mg/kg; p.o.; daily or twice daily from 27-41 days) shows effects on collagen-induced arthritis^[1].
PLX647 (30 mg/kg) results in significant inhibition of TRAP5b immunostaining and bone osteolysis. PLX647 (30 mg/kg BID) is able to prevent bone damage by the tumor cells^[1].

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

Animal Model:	Male C57BL/6 mice (mouse unilateral ureter obstruction model)^[1]
Dosage:	40 mg/kg
Administration:	P.o.; twice daily for 7 days
Result:	Resulted in reduction in the levels of F4/80+ macrophages by 77%.

Animal Model:	7-9 wk old Male DBA/1J mice (Mouse collagen-induced arthritis model)^[1]
Dosage:	20 mg/kg, 80 mg/kg
Administration:	P.o.; daily (20 mg/kg) from 27-41 days, twice daily (80 mg/kg) from 27-41 days
Result:	20 mg/kg PLX647 had no initial effect on the development of severe arthritis. However, starting on day 33, no further development of disease severity was recorded, and a 30% inhibition of the macroscopic signs of arthritis was evident in clinical score on day 41. Mice treated with 80 mg/kg BID PLX647 initially shows delayed development of severe arthritic signs. Starting on day 33, the signs of arthritis began to decrease in this treatment group, reaching a maximum reversal of 76% on day 41.

Molecular Weight

382.38

Formula

C₂₁H₁₇F₃N₄

CAS No.

873786-09-5

Appearance

Solid

Color

Light yellow to khaki

SMILES

FC(C1=CC=C(CNC2=NC=C(CC3=CNC4=NC=CC=C43)C=C2)C=C1)(F)F

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 : 25 mg/mL (65.38 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	2.6152 mL	13.0760 mL	26.1520 mL
5 mM	0.5230 mL	2.6152 mL	5.2304 mL
10 mM	0.2615 mL	1.3076 mL	2.6152 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

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 (6.54 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.54 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
(per animal)

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: 99.79%

Select Batch:

Data Sheet (274 KB) SDS (0 KB)

COA (247 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Zhang C, et al. Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5689-94. [Content Brief]

[2]. Louvet C, et al. Tyrosine kinase inhibitors reverse type 1 diabetes in nonobese diabetic mice. Proc Natl Acad Sci U S A. 2008 Dec 2;105(48):18895-900. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6152 mL	13.0760 mL	26.1520 mL	65.3800 mL
	5 mM	0.5230 mL	2.6152 mL	5.2304 mL	13.0760 mL
	10 mM	0.2615 mL	1.3076 mL	2.6152 mL	6.5380 mL
	15 mM	0.1743 mL	0.8717 mL	1.7435 mL	4.3587 mL
	20 mM	0.1308 mL	0.6538 mL	1.3076 mL	3.2690 mL
	25 mM	0.1046 mL	0.5230 mL	1.0461 mL	2.6152 mL
	30 mM	0.0872 mL	0.4359 mL	0.8717 mL	2.1793 mL
	40 mM	0.0654 mL	0.3269 mL	0.6538 mL	1.6345 mL
	50 mM	0.0523 mL	0.2615 mL	0.5230 mL	1.3076 mL
	60 mM	0.0436 mL	0.2179 mL	0.4359 mL	1.0897 mL

PLX647 Related Classifications

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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