BX-2819
BX-2819 is a Hsp90 inhibitor with an IC50 value of 41 nM. BX-2819 inhibits the proliferation of cancer cells. BX-2819 can significantly inhibit the growth of NCI-N87 and HT-29 tumors in nude mice.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 1184181-50-7
- 화학식: C21H24N4O4S
- 분자량:428.50
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- 순도&문서
- References
-
Help & FAQs
Biological Activity
|
HSP90 41 nM (IC50) |
HSP70 |
BX-2819 (0.001-10 μM, 16 h) can inhibit the expression of ErbB2 protein and significantly enhances the expression of Hsp70 in HT-29, OVCAR3 and SKBR3[1].
BX-2819 (0.001-10 μM, 72 h) can inhibit cell proliferation in SKBR3 (IC50=14 nM), SKOV3 (IC50 = 36 nM), 50 MKN45 (IC50=72 nM), NCI-N87 (IC50= 7 nM) tumor cancer cells[1].
BX-2819 (100 μM) has no significant cytotoxic effects on cells in HepG2 and RPTEC cells[1] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:NCI-N87, MKN-45
-
Concentration:0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM
-
Incubation Time:16 h
-
Result:Significantly inhibited the expression of ErbB2, Raf1 and c-Met proteins.
BX-2819 (2 mk/kg, intravenous injection (i.v.), single dose) shows relatively short serum half-life (t1/2=0.8 h), high clearance rate (CL=159 mL/min/kg), and large distribution volume (Vss=4.5 L) in rats[1].
Pharmacokinetic parameters of BX-2819 in rats (n = 4) [1]
| Dose（mg/kg） | Route | T1/2(h) | AUCinf(μg h/mL) | CL (mL/min) | Vss(L/kg) |
| 2 | iv | 0.8 | 0.23 | 159 | 4.5 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:SKOV3, HT-29 and NCI-N87 xenograft models in nude mice[1]
-
Dosage:100 mg/kg
-
Administration:Intraperitoneal injection (i.p.), twice a week
-
Result:Significantly inhibited ErbB2 expression, effectively inhibited Hsp90 for a long time, and enhanced Hsp70 expression.
Could enter the plasma after intraperitoneal injection.
Significantly decreased in tumor growth and final tumor burden.
Chemical Information
-
CAS No. 1184181-50-7
-
분자량 428.50
-
화학식 C21H24N4O4S
-
SMILES
CCOC(NCC1=CC=C(C=C1)N2C(NN=C2C3=C(C=C(C(C(C)C)=C3)O)O)=S)=O
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BX-2819 Related Classifications
HY-157085 Related Classifications
Powered by Bioz