咨询热线:

020-3107 8154

Vismodegib 维莫德吉; GDC-0449

Vismodegib (GDC-0449) 是一种具有口服活性的 hedgehog 抑制剂,IC50 值为 3 nM;还可抑制 P-gp 和 ABCG2 的活性,IC50 值分别为 3.0 μM 和 1.4 μM。

  • 货号:
    TK0457
  • 规格:
    1mg
    5mg
    10mg
    50mg
  • 价格:
    0.00

产品参数

CAS No.879085-55-9
生物活性Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively.
分子式C19H14Cl2N2O3S
分子量421.30
运输条件Room temperature in continental US; may vary elsewhere.
储存条件Powder -20°C 3 years
溶解性数据DMSO : 50 mg/mL (118.68 mM; Need ultrasonic) Ethanol : 3.33 mg/mL (7.90 mM; ultrasonic and warming and heat to 60°C)
体内研究Vismodegib is a novel small molecule HPI, often used for clinical trials. Vismodegib (0.3 to 75 mg/kg, p.o.) is highly efficacious in medulloblastoma allograft tumors. Vismodegib (> 46 mg/kg, p.o.) causes growth delay in patient-derived colorectal xenografts.
体外研究Vismodegib (HhAntag691) is an ABCG2 inhibitor and can increase the effective intracellular concentration of NSC 279836, another ABCG2 substrate, through blocking its export in HEK293 cells. Vismodegib (HhAntag691, 10 µM), resensitizes MDCKII/Pgp cells and MDCKII/MRP1 cells to NSC757 treatment. Vismodegib (25 μM or 50 μM) concentration dependently inhibits HCC and H1339 cells.
文献•J Exp Clin Cancer Res. 2019 Sep 13;38(1):404. •Oncogene. 2020 Jun;39(24):4711-4727. •Oncogene. 2020 Apr;39(16):3336-3353. •J Control Release. 2019 Apr 17;303:77-90. •Cancer Lett. 2018 Apr 28;420:195-207. •Oncogenesis. 2018 Mar 13;7(3):24. •Front Cell Dev Biol. 19 July 2021. •J Genet Genomics. 2018 May 20;45(5):237-246. •Drug Deliv Transl Res. 2015 Aug;5(4):407-23. •Prostate. 2021 Jan 27. •Dev Neurobiol. 2017 Dec;77(12):1385-1400. •Biomed J. 2020 Aug;43(4):368-374. •Bioorgan Med Chem. 2021, 116166. •Oncol Lett. 2019 Sep;18(3):3081-3091. •Hematology. 2022 Dec;27(1):1-10. •Parasitol Int. 2017 Oct;66(5):545-554. •Anticancer Drugs. 2018 Mar;29(3):208-215. •Research Square Preprint. 2022 Jan. •Research Square Preprint. 2020 Nov. •bioRxiv. 2019 Mar. •Patent. US20180263995A1.
纯度及产品资料98%