Dabrafenib

Dabrafenib
Artikelnummer Größe Datenblatt Manual SDB Lieferzeit Menge Preis
Cay16989-5 5 mg -

3 - 10 Werktage*

44,00 €
Cay16989-10 10 mg -

3 - 10 Werktage*

84,00 €
Cay16989-25 25 mg -

3 - 10 Werktage*

198,00 €
Cay16989-50 50 mg -

3 - 10 Werktage*

329,00 €
 
Dabrafenib is an ATP-competitive inhibitor of Raf kinases (IC50s = 0.64, 0.68, and 5 nM for... mehr
Produktinformationen "Dabrafenib"
Dabrafenib is an ATP-competitive inhibitor of Raf kinases (IC50s = 0.64, 0.68, and 5 nM for wild-type B-RAF kinase, mutant B-RAFV600E, and wild-type C-RAF kinase, respectively). It also inhibits the tyrosine kinase-like kinases ALK5 and LIMK1 (IC50s = 11 and 15 nM, respectively) and the calcium/calmodulin-dependent protein kinases SIK2 and PDK2 (IC50s = 27 and 57 nM, respectively), as well as NEK11, CK1, and BRK (IC50s = 20, 41, and 79 nM, respectively) in a panel of 270 kinases at 300 nM. Dabrafenib inhibits the growth of 16 cancer cell lines expressing mutant B-RAFV600E (GI50s = 50s = 50s = V600E, 133 cell lines expressing wild-type Ras and Raf, or 18 cell lines expressing mutant Ras (GI50s = >10 µM) in a panel of 195 cancer cell lines. Dabrafenib (8 nM) inhibits MAPK signaling, inhibiting phosphorylation of MEK and ERK, and activates caspase-3/7 in B-RAFV600E-expressing A375P melanoma cells but not in wild-type B-RAF-expressing human foreskin fibroblasts (EC200s =71 and >10,000 nM, respectively). It reduces tumor growth in an A375P mouse xenograft model when administered at doses ranging from 3 to 100 mg/kg. Formulations containing dabrafenib have been used in the treatment of B-RAFV600E-expressing cancers. Formal Name: N-[3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluoro-benzenesulfonamide. CAS Number: 1195765-45-7. Synonyms: GSK2118436. Molecular Formula: C23H20F3N5O2S2. Formula Weight: 519.6. Purity: >98%. Formulation: A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 1 mg/ml. lambdamax: 281, 333 nm. SMILES: FC1=C(C2=C(C3=CC=NC(N)=N3)SC(C(C)(C)C)=N2)C=CC=C1NS(C4=C(F)C=CC=C4F)(=O)=O. InChi Code: InChI=1S/C23H20F3N5O2S2/c1-23(2,3)21-30-18(19(34-21)16-10-11-28-22(27)29-16)12-6-4-9-15(17(12)26)31-35(32,33)20-13(24)7-5-8-14(20)25/h4-11,31H,1-3H3,(H2,27,28,29). InChi Key: BFSMGDJOXZAERB-UHFFFAOYSA-N.
Schlagworte: GSK2118436, N-[3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluoro-benzenesulfonamide
Hersteller: Cayman Chemical
Hersteller-Nr: 16989

Eigenschaften

Anwendung: B-Raf V600E inhibitor
MW: 519.6 D
Formel: C23H20F3N5O2S2
Reinheit: >98%
Format: Crystalline Solid

Datenbank Information

CAS : 1195765-45-7| Finde Alternativen
KEGG ID : K04365 | Finde Alternativen

Handhabung & Sicherheit

Lagerung: -20°C
Versand: -20°C (International: -20°C)
Signalwort: Warning
GHS-Piktogramme:
H-Sätze: H361, H373, H400, H411
P-Sätze: P201, P202, P260, P273, P280, P308+313, P314, P391, P405, P501
Achtung
Nur für Forschungszwecke und Laboruntersuchungen: Nicht für die Anwendung im oder am Menschen!
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