Cat. No.: HY-114323

PROTAC FLT-3 degrader 1

Name: PROTAC FLT-3 degrader 1
Brand: MedChemExpress
SKU: HY-114323
Price: 120.00 USD
Availability: InStock
Rating: 5 (1 reviews)

Customer Review

Based on 1 Customer Validation

PROTAC FLT-3 degrader 1 is an effective and selective FLT-3 PROTAC degrader with an IC₅₀ of 0.6 nM. PROTAC FLT-3 degrader 1 inhibits both FLT-3 and FLT-3 ITD mutants. PROTAC FLT-3 degrader 1 has the activity of anti-proliferation and induction of apoptosis, which can be used in the study of tumor.
(Pink: FLT-3 ligand (HY-168702); Blue: VHL ligand (HY-125845); Black: linker (HY-124380)).

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

Purity: 99.19%
CAS No.: 2230826-81-8
Formula: C₅₂H₆₁N₉O₉S₂
Molecular Weight:1020.23

Storage:

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

PROTAC FLT-3 degrader 1 Chemical Structure

CAS No.: 2230826-81-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC FLT-3 degrader 1 is an effective and selective FLT-3 PROTAC degrader with an IC₅₀ of 0.6 nM. PROTAC FLT-3 degrader 1 inhibits both FLT-3 and FLT-3 ITD mutants. PROTAC FLT-3 degrader 1 has the activity of anti-proliferation and induction of apoptosis, which can be used in the study of tumor^[1]. (Pink: FLT-3 ligand (HY-168702); Blue: VHL ligand (HY-125845); Black: linker (HY-124380)).

IC₅₀ & Target^[1]

STAT5

All PROTACs Isoforms :

All STAT Isoforms :

All MEK Isoforms :

All ERK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MOLM-14	IC₅₀	0.6 nM Compound: 54	Antiproliferative activity against human MOLM-14 cells Antiproliferative activity against human MOLM-14 cells	[PMID: 34656901]
MV4-11	IC₅₀	0.6 nM Compound: 54	Antiproliferative activity against human MV4-11 cells Antiproliferative activity against human MV4-11 cells	[PMID: 34656901]

In Vitro

PROTAC FLT-3 degrader 1 (0.05 nM-1 μM; 24 h) induces FLT-3 ITD protein degradation and inhibits downstream STAT-5, MEK and ERK phosphorylation, and has anti-proliferation and apoptosis-inducing activities in MV4-11 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

MV4-11 cells
Concentration:

0.05, 0.5 and 2 nM
Incubation Time:

24 h
Result:

Reduced the phosphorylation levels of STAT-5, MEK and ERK.

In Vivo

PROTAC FLT-3 degrader 1 (30 mg/kg; Intraperitoneal injection; 3 days) can degrade FLT-3 protein in mouse tumor model^[1].
Pharmacokinetic Analysis in Mouse^[1]

Route	Dose (mg/kg)	C_max (ng/mL)	T_max (hr)	t_1/2 (hr)	Plasma Protein Binding
i.p.	10	1069	2	2.31	98.0 %

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

Animal Model:

MV4-11 cells treated athymic mice^[1]
Dosage:

30 mg/kg
Administration:

Intraperitoneal injection (i.p.); 3 days
Result:

Did not cause any adverse effects.
Significantly decreased (approximately 60%) in total FLT-3 protein.
Suppressed the downstream signaling of FLT-3 ITD in tumor samples.

Chemical Information

CAS No. 2230826-81-8
Appearance Solid
Molecular Weight 1020.23
Formula C₅₂H₆₁N₉O₉S₂
Color White to light yellow
SMILES

O=C(N[C@@H](C(C)(C)C)C(N1[C@H](C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O)CCOCCOCCOC4=CC5=C(N6C(S5)=NC(C7=CC=C(NC(NC8=NOC(C(C)(C)C)=C8)=O)C=C7)=C6)C=C4
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 : 150 mg/mL (147.03 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

0.9802 mL

4.9009 mL

9.8017 mL

5 mM

0.1960 mL

0.9802 mL

1.9603 mL

10 mM

0.0980 mL

0.4901 mL

0.9802 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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: 7.5 mg/mL (7.35 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 7.5 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 (75.0 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: 7.5 mg/mL (7.35 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 7.5 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 (75.0 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: ≥ 7.5 mg/mL (7.35 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 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 (75.0 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Handling Instructions (2659 KB)

References

[1]. Burslem GM, et al. Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion. J Am Chem Soc. 2018 Dec 5;140(48):16428-16432. [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	0.9802 mL	4.9009 mL	9.8017 mL	24.5043 mL
	5 mM	0.1960 mL	0.9802 mL	1.9603 mL	4.9009 mL
	10 mM	0.0980 mL	0.4901 mL	0.9802 mL	2.4504 mL
	15 mM	0.0653 mL	0.3267 mL	0.6534 mL	1.6336 mL
	20 mM	0.0490 mL	0.2450 mL	0.4901 mL	1.2252 mL
	25 mM	0.0392 mL	0.1960 mL	0.3921 mL	0.9802 mL
	30 mM	0.0327 mL	0.1634 mL	0.3267 mL	0.8168 mL
	40 mM	0.0245 mL	0.1225 mL	0.2450 mL	0.6126 mL
	50 mM	0.0196 mL	0.0980 mL	0.1960 mL	0.4901 mL
	60 mM	0.0163 mL	0.0817 mL	0.1634 mL	0.4084 mL
	80 mM	0.0123 mL	0.0613 mL	0.1225 mL	0.3063 mL
	100 mM	0.0098 mL	0.0490 mL	0.0980 mL	0.2450 mL

Bioz

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

PROTAC FLT-3 degrader 1

Quizartinib

Fedratinib

PROTAC FAK degrader 1

Denfivontinib

AST 487

GMB-475

TG101209

SKLB4771

Mivavotinib

Quizartinib (Standard)

Fedratinib (Standard)

TG101209 (Standard)

All PROTACs Isoforms

All STAT Isoforms

All MEK Isoforms

All ERK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

PROTAC FLT-3 degrader 1

Quizartinib

Fedratinib

PROTAC FAK degrader 1

Denfivontinib

AST 487

GMB-475

TG101209

SKLB4771

Mivavotinib

Quizartinib (Standard)

Fedratinib (Standard)

TG101209 (Standard)

All PROTACs Isoforms

All STAT Isoforms

All MEK Isoforms

All ERK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PROTAC FLT-3 degrader 1 Related Classifications

HY-114323 Related Classifications

Bioz