MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)。

SAR405838

CAS No. : 1303607-60-4

MCE 國際站：SAR405838

產(chǎn)品活性：SAR405838 (MI-77301) 是 MI-773 的類似物，是一種高效、選擇性的 MDM2-p53 相互作用抑制劑，與 MDM2 結(jié)合的 K_i 值為 0.88 nM。SAR405838 具有強大的抗腫瘤活性。

研究領(lǐng)域：Apoptosis  |  Metabolic Enzyme/Protease

作用靶點：MDM-2/p53  |  E1/E2/E3 Enzyme  |  Apoptosis

In Vitro: SAR405838 (MI-77301) potently inhibits cell growth in cancer cell lines, including SJSA-1 (IC50, 0.092 μM), RS4;11 (IC50, 0.089 μM), LNCaP (IC50, 0.27 μM), and HCT-116 (IC50, 0.20 μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 (IC50, >10 μM), PC-3 (IC50, >10 μM), SW620 (IC50, >10 μM), and HCT-116 (p53-/-) (IC50, >20 μM) cells.
SAR405838 effectively induces apoptosis in the RS4;11 cell line. SAR405838 potently inhibits cell growth and induces dose-dependent apoptosis in the ABTR1 and ABTR2 sublines, albeit with modestly reduced potency compared with that in the control RS4;11 cell line.

In Vivo: At well-tolerated dose schedules, SAR405838 achieves either durable tumor regression or complete tumor growth inhibition in mouse xenograft models of SJSA-1 osteosarcoma, RS4;11 acute leukemia, LNCaP prostate cancer and HCT-116 colon cancer. Remarkably, a single oral dose of SAR405838 is sufficient to achieve complete tumor regression in the SJSA-1 model. In the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model, MI-773 (p.o.) effectively inhibits tumor growth in a dose-dependent manner (10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg, and 200 mg/kg,).

相關(guān)產(chǎn)品：Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  SY-5609  |  BRD4 Inhibitor-18  |  8α-Tigloyloxyhirsutinolide 13-O-acetate  |  AAPK-25  |  Dutasteride-¹³C₆  |  Oleic acid-¹³C  |  Anticancer agent 120  |  Abacavir sulfate  |  Meloxicam-d₃-1  |  Thailanstatin D  |  WSB1 Degrader 1  |  SB-218078  |  Toyocamycin  |  Sorafenib-d₄  |  Busulfan  |  PTC-028  |  Dinaciclib  |  CR-1-31-B  |  142I5  |  Farudodstat  |  Ecteinascidin 770  |  AT9283  |  Staurosporine  |  SNS-032  |  AZA1  |  Antitumor agent-96  |  Bleomycin A5  |  Xevinapant  |  Mangiferin  |  Cambinol

熱門產(chǎn)品線：重組蛋白  |  化合物庫  |  天然產(chǎn)物  |  熒光染料  |  PROTAC  |  同位素標(biāo)記物  |  寡核苷酸  |  抗體  |  點擊化學(xué)

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry