Cat. No.: HY-148794

Risvodetinib

(Synonyms: IkT-148009)

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Risvodetinib (IkT-148009) is an orally active, selective and brain-penetrant protein tyrosine kinase inhibitor, displaying excellent target efficacy against c-Abl1, c-Abl2/Arg with IC₅₀ values of 33 nM, 14 nM, respectively. Risvodetinib suppresses c-Abl activation and substantially protects dopaminergic neurons from degeneration in mouse models of both inherited and sporadic Parkinson’s disease (PD), which is promising for research in the field of PD.

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Pureté: 99.15%
CAS No.: 2031185-00-7
Formule: C₃₃H₃₄N₈O₂
Masse moléculaire:574.68

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Risvodetinib Chemical Structure

CAS No.: 2031185-00-7

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Activité biologique
- Description
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform Bcr-Abl :

Abl
Bcr-Abl

In Vivo

Risvodetinib (100 mg/kg, p.o., daily for 10 days) performs robust functional rescue and significant protection of dopaminergic (DA) neurons in the MPTP acute neurotoxicity mouse model^[1].
Risvodetinib (50 or 100 mg/kg, p.o., daily for 8 or 20 weeks) recovers nigrostriatal neurodegeneration and reduces phosphorylated α-synuclein in the mouse model of inherited PD^[1].
Risvodetinib (100 mg/kg, p.o., once a day, 5 times per week for 6 months) has an effective neuroprotection and reduces α-synuclein pathology in mouse model of sporadic PD^[1].

Pharmacokinetics of IkT-148009 in mouse plasma and brain^[1]

100 mg/kg per day	T_max (hours)	C_max (ng/mL)	AUC_0-last (ng·hour/mL)	AUC_0-inf (ng·hour/mL)	T_1/2 (hours)	Plasma/brain (ng/ml)	Bioavailability (%)	Brain:plasma (%)
Mean day 1 plasma	4	5060	37838	38000	2.6	-	58.6
Mean day 1 whole brain^*	2	98.1	1170	1200	3.8	-	-	2.7^†
Mean day 1 plasma/brain						3695/98.1-
Mean day 7 plasma/brain						5991/713		11.9^†

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

Animal Model:

MPTP neurotoxicity mouse model of PD^[1]
Dosage:

100 mg/kg
Administration:

p.o., daily for 10 days, behavioral tests performed on day 9
Result:

Protected from degeneration of nigrostriatal DA neurons in mouse brain and significantly reduced the MPTP-induced loss of dopamine and the loss of DOPAC, HVA, 3MT in behavioral assessments.

Animal Model:

Mouse model of inherited PD^[1]
Dosage:

50 or 100 mg/kg
Administration:

p.o., daily for 8 or 20 weeks
Result:

Significantly reduced the loss of nigrostriatal neurons and suppressed or partially reduced phosphorylated α-synuclein in the mouse brain region.

Animal Model:

α-Synuclein PFF progressive disease PD model of C57Bl/6 mice^[1]
Dosage:

100 mg/kg
Administration:

p.o., once a day, 5 days per week for 6 months
Result:

Prevented ≥85% of these nigrostriatal DA neurons from degeneration and suppressed markers of pathological α-synuclein in mouse brain.

Essai clinique

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

Chemical Information

CAS No. 2031185-00-7
Appearance Solid
Masse moléculaire 574.68
Formule C₃₃H₃₄N₈O₂
Color Light yellow to yellow
SMILES

O=C(C1=CC=C(CN2CCN(CC2)C)C=C1)NC3=CC=C(C)C(NC4=NC(C5=CN=CC(C6=C(C)C=NO6)=C5)=CC=N4)=C3
Synonyms

IkT-148009
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (174.01 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

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7401 mL

8.7005 mL

17.4010 mL

5 mM

0.3480 mL

1.7401 mL

3.4802 mL

10 mM

0.1740 mL

0.8700 mL

1.7401 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.35 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.35 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (4.35 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
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)
Instruction de manipulation (2659 KB)

Références

[1]. Karuppagounder SS, et al. The c-Abl inhibitor IkT-148009 suppresses neurodegeneration in mouse models of heritable and sporadic Parkinson's disease. Sci Transl Med. 2023 Jan 18;15(679):eabp9352. [Content Brief]

[2]. Werner MH, et al. Preparation of N-[3-[[4-(2-pyridyl)pyrimidin-2-yl]amino]phenyl]-4-[(piperazin-1-yl)methyl]benzamide derivatives as inhibitors of kinases: World Intellectual Property Organization, WO2016172528. 2016-10-27.

[3]. WHO Drug Information-World Health Organization (WHO).

[4]. Werner MH, Olanow CW. Parkinson's Disease Modification Through Abl Kinase Inhibition: An Opportunity[J]. Mov Disord. 2022 Jan;37(1):6-15. [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	1.7401 mL	8.7005 mL	17.4010 mL	43.5025 mL
	5 mM	0.3480 mL	1.7401 mL	3.4802 mL	8.7005 mL
	10 mM	0.1740 mL	0.8700 mL	1.7401 mL	4.3502 mL
	15 mM	0.1160 mL	0.5800 mL	1.1601 mL	2.9002 mL
	20 mM	0.0870 mL	0.4350 mL	0.8700 mL	2.1751 mL
	25 mM	0.0696 mL	0.3480 mL	0.6960 mL	1.7401 mL
	30 mM	0.0580 mL	0.2900 mL	0.5800 mL	1.4501 mL
	40 mM	0.0435 mL	0.2175 mL	0.4350 mL	1.0876 mL
	50 mM	0.0348 mL	0.1740 mL	0.3480 mL	0.8700 mL
	60 mM	0.0290 mL	0.1450 mL	0.2900 mL	0.7250 mL
	80 mM	0.0218 mL	0.1088 mL	0.2175 mL	0.5438 mL
	100 mM	0.0174 mL	0.0870 mL	0.1740 mL	0.4350 mL

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Risvodetinib

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Voir tous les produits spécifiques à Isoform Bcr-Abl

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Risvodetinib

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Voir tous les produits spécifiques à Isoform Bcr-Abl

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Risvodetinib Related Classifications

HY-148794 Related Classifications