1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR FLT3 Bcr-Abl
  3. Ruserontinib

Ruserontinib  (Synonyms: SKLB1028)

Cat. No.: HY-120590 Purity: 99.82%
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Ruserontinib (SKLB1028) is an orally active multikinase inhibitor of EGFR, FLT3 and Abl, with an IC50 value of 55 nM for human FLT3, and has antitumor activity.

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

Ruserontinib Chemical Structure

Ruserontinib Chemical Structure

CAS No. : 1350544-93-2

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10 mg USD 240 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Ruserontinib (SKLB1028) is an orally active multikinase inhibitor of EGFR, FLT3 and Abl, with an IC50 value of 55 nM for human FLT3, and has antitumor activity[1].

In Vitro

Ruserontinib (SKLB1028) can significantly inhibit the growth of mf4-11 cells expressing FLT3-ITD with IC50 value of 0.002 μM, inhibit the proliferation of RS4-11 cells expressing wt-FLT3 with IC50 value of 0.790 μM, and inhibit Ba The IC50 value for the growth of /F3 cells is 0.01 μM, and the IC50 value for inhibiting the growth of K562 cells expressing the Bcr-Abl mutant is 0.190 μM[1].
Ruserontinib (SKLB1028) (0-100 nM, 20 h) causes a dose-dependent decrease in the level of pro-caspase-3 in MV4-11 cells, while a dose-dependent increase in the level of the cleaved caspase-3 fragment, and can be dose-dependent Inhibits phosphorylation of STAT5 and Erk1/2 in a dependent manner[1].

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

In Vivo

Ruserontinib (SKLB1028) (5-70 mg/kg, orally once daily, 18 days) have anti-tumor effect in MV4-11 and K562 xenograft NOD-SCID models[1].

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

Animal Model: MV4-11 and K562 xenograft NOD-SCID models[1]
Dosage: 5, 10, 20 mg/kg,70 mg/kg
Administration: orally once daily, 18 days
Result: Prevented tumor growth at a dose of 5 mg/kg, and caused rapid and complete tumor regression in both groups of mice at a dose of 10 or 20 mg/kg.
Significantly inhibited the proliferation and induced apoptosis of MV4-11 and K562 cells at a dose of 70 mg/kg.
Clinical Trial
Molecular Weight

443.55

Formula

C24H29N9

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C4N=C(N(C4=N3)C(C)C)NC5=CC=CN=C5

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 250 mg/mL (563.63 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 2.2545 mL 11.2727 mL 22.5454 mL
5 mM 0.4509 mL 2.2545 mL 4.5091 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 2.2545 mL 11.2727 mL 22.5454 mL 56.3634 mL
5 mM 0.4509 mL 2.2545 mL 4.5091 mL 11.2727 mL
10 mM 0.2255 mL 1.1273 mL 2.2545 mL 5.6363 mL
15 mM 0.1503 mL 0.7515 mL 1.5030 mL 3.7576 mL
20 mM 0.1127 mL 0.5636 mL 1.1273 mL 2.8182 mL
25 mM 0.0902 mL 0.4509 mL 0.9018 mL 2.2545 mL
30 mM 0.0752 mL 0.3758 mL 0.7515 mL 1.8788 mL
40 mM 0.0564 mL 0.2818 mL 0.5636 mL 1.4091 mL
50 mM 0.0451 mL 0.2255 mL 0.4509 mL 1.1273 mL
60 mM 0.0376 mL 0.1879 mL 0.3758 mL 0.9394 mL
80 mM 0.0282 mL 0.1409 mL 0.2818 mL 0.7045 mL
100 mM 0.0225 mL 0.1127 mL 0.2255 mL 0.5636 mL
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Ruserontinib 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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