Debio 0932

小分子

黛比奥0932

F85396 | 2-(6-(Dimethylamino)benoz[d][1,3]dioxol-5-yl-thio)-1-(2-neopentylamino)ethyl)-1H-imidazo[4,5-c]pyridin-4-amine | 1H-IMIDAZO(4,5-C)PYRIDINE-1-ETHANAMINE, 4-AMINO-2-((6-(DIMETHYLAMINO)-1,3-BENZODIOXOL-5-YL)THIO)-N-(2,2-DIMETHYLPROPYL)- | BDBM504396

Debio 0932

D650628-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

Debio 0932 (CUDC-305) is an orally active HSP90 inhibitor, with IC 50 s of 100 and 103 nM for HSP90α and HSP90β, respectively In Vitro Debio 0932 is an orally active HSP90 inhibitor, with IC 50 s of 100 and 103 nM for HSP90α and HSP90β, respectively. Debio 0932 (CUDC-305) binds to the tumor HSP90 complex with a mean IC 50 of 48.8 nM. Debio 0932 (1 μM) promotes degradation of multiple HSP90 client proteins in cancer cell lines. Debio 0932 also shows inhibitory activities against the proliferation of 40 cancer cell lines (containing 34 solid and 6 hematologic tumor-derived lines) with an IC 50 ranging from 40 to 900 nM (mean IC 50 , 220 nM). Debio 0932 strongly binds to cancer-derived HSP90 complex with an IC 50 of 61.2 nM in H1975 cells and 74.2 nM in H1993 cells, respectively. Debio 0932 (CUDC-305, 1 μM) durably induces oncoprotein degradation in NSCLC cell lines with mutations that can confer resistance to erlotinib. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Debio 0932 (CUDC-305, 30 mg/kg, p.o.) exhibits favorable pharmacokinetic profiles in tumor-bearing nude mice. Debio 0932 (160 mg/kg, p.o.) causes degradation of HSP90 client proteins, suppresses tumor growth, and also prolongs survival in various animal models of U87MG glioblastoma. Debio 0932 (40, 80, or 160 mg/kg, p.o.) also dose-dependently inhibits tumor growth in the U87MG s.c. tumor model by every-other-day (q2d) dosing . Debio 0932 (80 mg/kg, p.o.) significantly alleviates psoriasis by day 11 and decreases epidermal thickness in psoriasis xenograft transplantation model. Debio 0932 (CUDC-305) is able to cross the blood-brain barrier. Debio 0932 (80, 120, and 160 mg/kg, p.o.) shows dose-dependent inhibition of tumor growth in the H1975 subcutaneous tumor model. Debio 0932 (160 mg/kg, p.o.) also promotes antitumor activity in the erlotinib-resistant H1975 subcutaneous tumor model. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:HSP90α 100 nM (IC 50 ) HSP90β 103 nM (IC 50 )

Debio 0932（CUDC-305）是一种口服活性 HSP90 抑制剂，对 HSP90α 和 HSP90β 的 IC 50 s 分别为 100 和 103 nM。

1061318-81-7

C22H30N6O2S

442.58 g/mol

44156921

CC(C)(C)CNCCN1C2=C(C(=NC=C2)N)N=C1SC3=CC4=C(C=C3N(C)C)OCO4

2-[[6-(dimethylamino)-1,3-benzodioxol-5-yl]sulfanyl]-1-[2-(2,2-dimethylpropylamino)ethyl]imidazo[4,5-c]pyridin-4-amine

1S/C22H30N6O2S/c1-22(2,3)12-24-8-9-28-14-6-7-25-20(23)19(14)26-21(28)31-18-11-17-16(29-13-30-17)10-15(18)27(4)5/h6-7,10-11,24H,8-9,12-13H2,1-5H3,(H2,23,25)

RVJIQAYFTOPTKK-UHFFFAOYSA-N

CC(C)(C)CNCCN1C2=C(C(=NC=C2)N)N=C1SC3=CC4=C(C=C3N(C)C)OCO4

44156921

DMSO : 75 mg/mL (169.46 mM; Need ultrasonic)

2

8

8

442.215 Da

442.215 Da

116.000 Ų

31

0

591.000

0

1

3.600