2. Stem Cell/Wnt JAK/STAT Signaling Epigenetics Protein Tyrosine Kinase/RTK Apoptosis
  3. JAK FLT3 Apoptosis
  4. JAK2/FLT3-IN-1 TFA

JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity.

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

JAK2/FLT3-IN-1 TFA Chemical Structure

JAK2/FLT3-IN-1 TFA Chemical Structure

CAS No. : 2928093-29-0

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Solid + Solvent
10 mM * 1 mL in Water
ready for reconstitution
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10 mM * 1 mL in Water USD 960 In-stock
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10 mg USD 1250 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of JAK2/FLT3-IN-1 TFA:

JAK2/FLT3-IN-1 TFA Related Antibodies

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Description

JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity[1].

IC50 & Target

JAK1

26 nM (IC50)

JAK2

0.7 nM (IC50)

JAK3

39 nM (IC50)

FLT3

4 nM (IC50)

In Vitro

JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) (TFA) down-regulates p-FLT3 in a dose-dependent manner[1].
JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA) has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells[1].
JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA) strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells[1].

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

JAK2/FLT3-IN-1 TFA Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4-11 and SET-2 cells
Concentration: 0.008, 0.04, 0.2, 1 μM
Incubation Time: For 2 hours
Result: Down-regulated p-FLT3 in a dose-dependent manner from 0.008 to 1 μM.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 5, 10, 50, 100 nM
Incubation Time: For 2 hours
Result: Had a dose-dependent effect on the induction of apoptosis in the MV4-11 cells.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 5, 10, 50, 100 nM
Incubation Time: For 2 hours
Result: Induced cell cycle arrest with a G1/G0 percentage of 85% at 100 nM.
In Vivo

JAK2/FLT3-IN-1 (30 and 60 mg/kg/day; p.o.; for 14 days) (TFA) exhibits significant antitumor effects[1].

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

Animal Model: NOD/SCID mouse models[1]
Dosage: 30 and 60 mg/kg
Administration: Oral administration; daily; for 14 days
Result: Exhibited significant antitumor effects.
The tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model.
Molecular Weight

581.61

Formula

C27H35F4N7O3
CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

OCCN(C1CCN(C2=CC=C(NC3=NC=C(C)C(C4=CN(C(C)C)N=C4)=N3)C=C2F)CC1)C.O=C(O)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 33.33 mg/mL (57.31 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7194 mL 8.5968 mL 17.1937 mL
5 mM 0.3439 mL 1.7194 mL 3.4387 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.77%

COA (247 KB) HNMR (126 KB) RP-HPLC (186 KB) LCMS (110 KB)

Handling Instructions (2659 KB)
References

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.7194 mL 8.5968 mL 17.1937 mL 42.9841 mL
5 mM 0.3439 mL 1.7194 mL 3.4387 mL 8.5968 mL
10 mM 0.1719 mL 0.8597 mL 1.7194 mL 4.2984 mL
15 mM 0.1146 mL 0.5731 mL 1.1462 mL 2.8656 mL
20 mM 0.0860 mL 0.4298 mL 0.8597 mL 2.1492 mL
25 mM 0.0688 mL 0.3439 mL 0.6877 mL 1.7194 mL
30 mM 0.0573 mL 0.2866 mL 0.5731 mL 1.4328 mL
40 mM 0.0430 mL 0.2149 mL 0.4298 mL 1.0746 mL
50 mM 0.0344 mL 0.1719 mL 0.3439 mL 0.8597 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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JAK2/FLT3-IN-1 TFA 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.

Keywords:

JAK2/FLT3-IN-12928093-29-0JAKFLT3ApoptosisJanus kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3orallyanti-cancercyclearrestG1/G0MV4-11Inhibitorinhibitorinhibit

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