RSH-7
Based on 1 Customer Validation
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.74%
- CAS No.: 2764609-97-2
- 화학식: C22H25FN8O
- 분자량:436.49
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
IC50: 47 nM (BTK); 12 nM (FLT3)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| JeKo-1 | IC50 |
17 nM
Compound: RSH-7
|
Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
|
[PMID: 36399923] |
| K562 | IC50 |
930 nM
Compound: RSH-7
|
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
|
[PMID: 36399923] |
| MOLT-4 | IC50 |
11 nM
Compound: RSH-7
|
Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
|
[PMID: 36399923] |
| MV4-11 | IC50 |
3 nM
Compound: RSH-7
|
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
|
[PMID: 36399923] |
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 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.
-
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.
-
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.
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.
Chemical Information
-
CAS No. 2764609-97-2
-
Appearance Solid
-
분자량 436.49
-
화학식 C22H25FN8O
-
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
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
-
Data Sheet (275 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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. 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 |