(S)-3-Hydroxy Midostaurin
Based on 1 Customer Validation
(S)-3-Hydroxy Midostaurin ((S)-CGP52421) is a potent kinases inhibitor with IC50 values of <400 nM for 13 kinases (VEGFR-2, TRK-A, FLT3, et). (S)-3-Hydroxy Midostaurin is a minor metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (S)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML).
For research use only. We do not sell to patients.
- Purity : 96.07%
- CAS No.: 945260-14-0
- Formula: C35H30N4O5
- Molecular Weight:586.64
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
530 nM
Compound: CGP-52421
|
Toxicity against human A375 cells after 72 hrs by cell titer-blue assay
Toxicity against human A375 cells after 72 hrs by cell titer-blue assay
|
[PMID: 19654408] |
| MV4-11 | IC50 |
64 nM
Compound: CGP-52421
|
Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay
Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay
|
[PMID: 19654408] |
| RS4-11 | IC50 |
160 nM
Compound: CGP-52421
|
Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
|
[PMID: 19654408] |
| RS4-11 | IC50 |
350 nM
Compound: CGP-52421
|
Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
|
[PMID: 19654408] |
In Vitro
(S)-3-Hydroxy Midostaurin ((S)-CGP52421; compound 4) has IC50 values in the range of 200-400 nM against the ITD and D835Y mutants and low micromolar activity against the wild-type enzyme[1].
The epimeric mixture of metabolites ((R)-3-Hydroxy Midostaurin + (S)-3-Hydroxy Midostaurin) substantially inhibits the proliferation of only the Tel-PDGFRβ (GI50=63 nM), KIT D816V (GI50=320 nM), and FLT3-ITD (GI50=650 nM) BaF3 cell lines, while the wild-type cells are relatively insensitive[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
-
CAS No. 945260-14-0
-
Appearance Solid
-
Molecular Weight 586.64
-
Formula C35H30N4O5
-
Color White to off-white
-
SMILES
O[C@@H]1NC(C2=C1C(C3=C4C=CC=C3)=C5N4[C@]6(C)[C@@H]([C@@H](C[C@](O6)([H])N7C5=C2C8=C7C=CC=C8)N(C(C9=CC=CC=C9)=O)C)OC)=O
-
Synonyms
(S)-CGP52421
-
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
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(S)-3-Hydroxy Midostaurin Related Classifications
HY-108263A Related Classifications
Powered by Bioz