MI-773 (SAR405838)

Name: MI-773 (SAR405838)
Brand: Selleck Chemicals
SKU: S7649
Rating: 5 (4 reviews)

For research use only. Not for use in humans.

Catalog No.S7649

4 publications

Molecular Weight(MW): 562.50

MI-773 (SAR405838) is an orally available MDM2 antagonist with K_i of 0.88 nM. Phase 1.

Selleck's MI-773 (SAR405838) has been cited by 4 publications

EMBO J, 2019, 38(20):e102096

PubMed: 31483066 ( click the link to review the publication )

Cell Chem Biol, 2018, 25(6):761-774

PubMed: 29681526 ( click the link to review the publication )

Oncotarget, 2017, 8(26):43008-43022

PubMed: 28498808 ( click the link to review the publication )

Oncotarget, 2016, 7(50):82757-82769

PubMed: 27764791 ( click the link to review the publication )

1 Customer Review

A panel of four NB cell lines were seeded in six-well plates with indicated concentrations of SAR405838 and agar, and grown for 2 to 3 weeks. Cells were stained with crystal violet for 4 hours. Colonies were counted and colony numbers were represented as % vehicle ± S.D. with P < 0.05 (*), P < 0.01 (**) or P < 0.001 (***) (Student's t-test, two-tailed) as indicated.

Oncotarget, 2016, 7(50):82757-82769. MI-773 (SAR405838) purchased from Selleck.

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Biological Activity

Description

MI-773 (SAR405838) is an orally available MDM2 antagonist with K_i of 0.88 nM. Phase 1.

Targets

p53 ^[1]	MDM2 ^[1] (Cell-free assay)
	0.88 nM(Ki)

In vitro

MI-773 binds to MDM2 with Ki of 0.88 nM. MI-773 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. ^[1]

In vivo

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,). ^[1]

Protocol

Kinase Assay:^[1]	- Collapse Fluorescence-polarization binding assay: Binding afﬁnities of MDM2 inhibitors and p53 peptide to MDM2 protein are determined using an Fluorescence-polarization (FP) binding assay. Binding afﬁnities of MI-773 to Bcl-2, Bcl-xL, Mcl-1, and β-catenin are determined using a competitive FP-based assay, and its binding afﬁnity to MDMx is determined using Biolayer Interferometry technology.
Cell Research:^[1]	- Collapse Cell lines: SJSA-1, RS4;11, LNCaP, SAOS-2, PC-3, SW620, HCT-116, and HCT-116 (p53^-/-) cells Concentrations: 100 μM Incubation Time: ~48 h Method: Cell growth inhibition activity is determined in a water-soluble tetrazolium-based assay. Cell death is measured by trypan blue staining and apoptosis is determined using an Annexin V-FLUOS staining kit. (Only for Reference)
Animal Research: ^[1]	- Collapse Animal Models: SCID mice with SJSA-1 osteosarcoma (females), acute lymphoblastic leukemia RS4;11 (females), LNCaP prostate cancer (males), or HCT-116 colon cancer (females) xenograft model Formulation: 10% PEG400: 3% Cremophor: 87% PBS, or 2% TPGS: 98% PEG200 Dosages: 200 mg/kg Administration: p.o. (Only for Reference)

References

[1] Wang S, et al. Cancer Res. 2014, 74(20), 5855-5865.

Solubility (25°C)

In vitro	DMSO	100 mg/mL (177.77 mM)
	Ethanol	31 mg/mL warmed (55.11 mM)
	Water	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight	562.50
Formula	C₂₉H₃₄Cl₂FN₃O₃
CAS No.	1303607-60-4
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	CC(C)(C)CC1NC(C(C2=CC=CC(=C2F)Cl)C13C(=O)NC4=C3C=CC(=C4)Cl)C(=O)NC5CCC(O)CC5

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MI-773 (SAR405838)