Art. -Nr.: HY-18986

SAR405838

(Synonyms: MI-77301)

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

SAR405838 (MI-77301), an analog of MI-773, is a highly potent and selective MDM2-p53 interaction inhibitor. SAR405838 binds to MDM2 with a K_i of 0.88 nM. SAR405838 induces apoptosis and has potent antitumor activity.

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Reinheit: 98.84%
CAS. Nr.: 1303607-60-4
Formel: C₂₉H₃₄Cl₂FN₃O₃
Molecular Weight:562.50

Speicherung:

-20°C, sealed storage, away from moisture

* The compound is unstable in solutions, freshly prepared is recommended.

SAR405838 Chemical Structure

CAS. Nr.: 1303607-60-4

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	GI₅₀	38 μM Compound: MI-77301	Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis	[PMID: 29691156]
HCT-116	GI₅₀	6 μM Compound: MI-77301	Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis	[PMID: 29691156]
HCT-116	IC₅₀	100 nM Compound: 10, SAR405838, MI-77301	Cytotoxicity against human HCT116 cells Cytotoxicity against human HCT116 cells	[PMID: 25396320]
HCT-116	IC₅₀	227 nM Compound: III; MI-773	Antiproliferative activity against human HCT-116 cells incubated for 4 days by CCK8 assay Antiproliferative activity against human HCT-116 cells incubated for 4 days by CCK8 assay	[PMID: 38581730]
LNCaP	IC₅₀	100 nM Compound: 10, SAR405838, MI-77301	Cytotoxicity against human LNCAP cells Cytotoxicity against human LNCAP cells	[PMID: 25396320]
MOLM-13	IC₅₀	115 nM Compound: III; MI-773	Antiproliferative activity against human MOLM-13 cells incubated for 2 days by CCK8 assay Antiproliferative activity against human MOLM-13 cells incubated for 2 days by CCK8 assay	[PMID: 38581730]
RS4-11	IC₅₀	100 nM Compound: 10, SAR405838, MI-77301	Cytotoxicity against human RS4:11 cells Cytotoxicity against human RS4:11 cells	[PMID: 25396320]
SJSA-1	IC₅₀	100 nM Compound: 10, SAR405838, MI-77301	Cytotoxicity against human SJSA1 cells Cytotoxicity against human SJSA1 cells	[PMID: 25396320]
SJSA-1	IC₅₀	214 nM Compound: SAR299155	Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum	[PMID: 24456472]
SJSA-1	IC₅₀	214 nM Compound: SAR299155	Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum	[PMID: 24601644]

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^[1].
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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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,)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1303607-60-4
Appearance Solid
Molecular Weight 562.50
Formel C₂₉H₃₄Cl₂FN₃O₃
Color White to off-white
SMILES

O=C([C@H](N[C@H]1CC(C)(C)C)[C@H](C2=CC=CC(Cl)=C2F)[C@@]31C(NC4=C3C=CC(Cl)=C4)=O)N[C@@H]5CC[C@@H](O)CC5
Synonyms

MI-77301
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture

* The compound is unstable in solutions, freshly prepared is recommended.

Publications (4)

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Clin Transl Med

Oncogenic driver and therapeutic target: Prolactin signalling axis in retroperitoneal sarcoma. [Abstract]

2026 May;16(5):e70669. PMID: 42083506
Clin Transl Med

USP7 inhibitors suppress tumour neoangiogenesis and promote synergy with immune checkpoint inhibitors by downregulating fibroblast VEGF. [Abstract]

2024 Apr;14(4):e1648. PMID: 38602256
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (177.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7778 mL

8.8889 mL

17.7778 mL

5 mM

0.3556 mL

1.7778 mL

3.5556 mL

10 mM

0.1778 mL

0.8889 mL

1.7778 mL

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.44 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wang S, et al. SAR405838: an optimized inhibitor of MDM2-p53 interaction that induces complete and durable tumor regression. Cancer Res. 2014 Oct 15;74(20):5855-5865. [Content Brief]

[2]. Hoffman-Luca CG, et al. Elucidation of Acquired Resistance to Bcl-2 and MDM2 Inhibitors in Acute Leukemia In Vitro and In Vivo. Clin Cancer Res. 2015 Jun 1;21(11):2558-2568. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7778 mL	8.8889 mL	17.7778 mL	44.4444 mL
	5 mM	0.3556 mL	1.7778 mL	3.5556 mL	8.8889 mL
	10 mM	0.1778 mL	0.8889 mL	1.7778 mL	4.4444 mL
	15 mM	0.1185 mL	0.5926 mL	1.1852 mL	2.9630 mL
	20 mM	0.0889 mL	0.4444 mL	0.8889 mL	2.2222 mL
	25 mM	0.0711 mL	0.3556 mL	0.7111 mL	1.7778 mL
	30 mM	0.0593 mL	0.2963 mL	0.5926 mL	1.4815 mL
	40 mM	0.0444 mL	0.2222 mL	0.4444 mL	1.1111 mL
	50 mM	0.0356 mL	0.1778 mL	0.3556 mL	0.8889 mL
	60 mM	0.0296 mL	0.1481 mL	0.2963 mL	0.7407 mL
	80 mM	0.0222 mL	0.1111 mL	0.2222 mL	0.5556 mL
	100 mM	0.0178 mL	0.0889 mL	0.1778 mL	0.4444 mL

Keywords

SAR405838

4 Cited Publications

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SAR405838

MCE Bioactive Compound Library

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) SAR405838

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SAR405838

MCE Bioactive Compound Library

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) SAR405838

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SAR405838 Related Classifications

HY-18986 Related Classifications