Cat. No.: HY-120590

Ruserontinib

(Synonyms: SKLB1028)

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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.

Purity: 99.32%
CAS No.: 1350544-93-2
Formula: C₂₄H₂₉N₉
Molecular Weight:443.55

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Ruserontinib Chemical Structure

CAS No.: 1350544-93-2

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

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].

All EGFR Isoforms :

All Bcr-Abl Isoforms :

Abl
Bcr-Abl

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1350544-93-2
Appearance Solid
Molecular Weight 443.55
Formula C₂₄H₂₉N₉
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
Synonyms

SKLB1028
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2545 mL

11.2727 mL

22.5454 mL

5 mM

0.4509 mL

2.2545 mL

4.5091 mL

10 mM

0.2255 mL

1.1273 mL

2.2545 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, 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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Z-X Cao, et al. SKLB1028, a novel oral multikinase inhibitor of EGFR, FLT3 and Abl, displays exceptional activity in models of FLT3-driven AML and considerable potency in models of CML harboring Abl mutants. Leukemia. 2012 Aug;26(8):1892-5. [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, 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

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All EGFR Isoforms

All Bcr-Abl Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Ruserontinib Related Classifications

HY-120590 Related Classifications