1. Protein Tyrosine Kinase/RTK
  2. Btk FLT3
  3. RSH-7

RSH-7 is a potent BTK and FLT3 inhibitor with IC50s of 47, 12 nM, respectively. RSH-7 induces apoptosis and shows antiproliferative activities. RSH-7 inhibits BTK and FLT3 signaling and shows anti-tumor activity.

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RSH-7 Chemical Structure

RSH-7 Chemical Structure

CAS No. : 2764609-97-2

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Based on 1 publication(s) in Google Scholar

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Description

RSH-7 is a potent BTK and FLT3 inhibitor with IC50s of 47, 12 nM, respectively. RSH-7 induces apoptosis and shows antiproliferative activities. RSH-7 inhibits BTK and FLT3 signaling and shows anti-tumor activity[1].

IC50 & Target

IC50: 47 nM (BTK); 12 nM (FLT3)[1]

In Vitro

RSH-7 (1-1000 nM; 72 h) shows antiproliferative activities with IC50s of 17, 3, 11, 930 nM for Jeko-1, MV-4-11, Molt4, K562 cells, respectively[1].
RSH-7 (30, 150, 750 nM; 72 h) decreases the expression of p-BTK (TYR223), p-PLCγ(Tyr1217), p-FLT3 (Tyr589), p-STAT5 (TYR694) in a dose-dependent manner[1].
RSH-7 (30, 150, 750 nM; 72 h) induces apoptosis and increases the expression of BAX, p53, cleaved caspase 3 in a dose dependen manner in jeko-1 cells[1].

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

Cell Viability Assay[1]

Cell Line: Jeko-1, MV-4-11, Molt4, K562 cells
Concentration: 1-1000 nM
Incubation Time: 72 h
Result: Showed antiproliferative activities with IC50s of 17, 3, 11, 930 nM for Jeko-1, MV-4-11, Molt4, K562 cells, respectively.

Western Blot Analysis[1]

Cell Line: jeko-1 cells
Concentration: 30, 150, 750 nM
Incubation Time: 72 h
Result: Reduced both BTK, PLCγ2, FLT3 and STAT5 phosphorylation in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: jeko-1 cells
Concentration: 30, 150, 750 nM
Incubation Time: 72 h
Result: Dose-dependently induced cell apoptosis and upregulated the expression of pro-apoptotic protein BAX, p53, cleaved caspase 3.
In Vivo

RSH-7 (25, 50 mg/kg; i.p.; daily for 16 days) shows anti-tumor activity with significantly and dose-dependently suppresses the tumor growth in mouse[1].

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

Animal Model: Female NOD/SCID mice (jeko-1 cell-inoculated xenograft NOD/SCID mice models)[1]
Dosage: 25, 50 mg/kg
Administration: I.p.; daily for 16 days
Result: Suppressed tumor growth in a dose-dependent manner, with tumor growth inhibition (TGI) values of 66.95% and 79.78% at doses of 25 and 50 mg/kg,
Animal Model: Female NOD/SCID mice (MV4-11 cell-inoculated xenograft NOD/SCID mice models)[1]
Dosage: 10, 20 mg/kg
Administration: I.p.; daily for 21 days
Result: Significantly and dose-dependently suppressed the tumor growth with the TGI rates of 74.23% and 94.84% at the dosage of 10 and 20 mg/kg, respectively.
Molecular Weight

436.49

Formula

C22H25FN8O

CAS No.
Appearance

Solid

Color

Gray to dark gray

SMILES

CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC(NC4=C(C=CC=C4)C(NN)=O)=C(C=N3)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (190.91 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 2.2910 mL 11.4550 mL 22.9100 mL
5 mM 0.4582 mL 2.2910 mL 4.5820 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
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. 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
DMSO 1 mM 2.2910 mL 11.4550 mL 22.9100 mL 57.2751 mL
5 mM 0.4582 mL 2.2910 mL 4.5820 mL 11.4550 mL
10 mM 0.2291 mL 1.1455 mL 2.2910 mL 5.7275 mL
15 mM 0.1527 mL 0.7637 mL 1.5273 mL 3.8183 mL
20 mM 0.1146 mL 0.5728 mL 1.1455 mL 2.8638 mL
25 mM 0.0916 mL 0.4582 mL 0.9164 mL 2.2910 mL
30 mM 0.0764 mL 0.3818 mL 0.7637 mL 1.9092 mL
40 mM 0.0573 mL 0.2864 mL 0.5728 mL 1.4319 mL
50 mM 0.0458 mL 0.2291 mL 0.4582 mL 1.1455 mL
60 mM 0.0382 mL 0.1909 mL 0.3818 mL 0.9546 mL
80 mM 0.0286 mL 0.1432 mL 0.2864 mL 0.7159 mL
100 mM 0.0229 mL 0.1146 mL 0.2291 mL 0.5728 mL
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RSH-7 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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RSH-7
Cat. No.:
HY-151961
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