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  3. Mobocertinib succinate

Mobocertinib succinate  (Synonyms: TAK-788 succinate; AP32788 succinate)

Cat. No.: HY-135815A Purity: 99.61%
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Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research.

For research use only. We do not sell to patients.

Mobocertinib succinate Chemical Structure

Mobocertinib succinate Chemical Structure

CAS No. : 2389149-74-8

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mg USD 60 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Mobocertinib succinate:

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Description

Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research[1][2].

IC50 & Target[1]

EGFR exon 20 insertion

 

HER2

 

EGFR (WT)

 

In Vitro

Mobocertinib succinate (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC50 of 21 nM[1].
Mobocertinib succinate (2 h) potently inhibits EGFR with common activating mutations (HCC827 (D), HCC4011 (L)) or with a T790M mutation (H1975 (LT)) more potently than WT EGFR (A431 (WT))[1].
Mobocertinib succinate (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells[1].
Mobocertinib succinate (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling[1].
Mobocertinib succinate (0.01, 0.1 and 1 μM; 6 h) inhibits HER2 signaling in H1781 (HER2 Exon 20G776>VC), Ba/F3 (HER2 exon 20YVMA) cells[2].

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

Cell Viability Assay[1]

Cell Line: LU0387 (NPH) cells
Concentration: 1.5 nM-10 μM
Incubation Time: 7 days
Result: Showed good inhibition activity for LU0387 (NPH) cells with IC50 of 21 nM.

Cell Viability Assay[1]

Cell Line: A431 (WT), HCC827 (D), HCC4011 (L), H1975 (LT) cells
Concentration:
Incubation Time: 2 h
Result: Inhibited EGFR with common activating mutations of HCC827 (D), HCC4011 (L) cells and T790M mutation of H1975 (LT) with IC50s of 4, 1.3 and 9.8 nM respectively, which more potently than WT EGFR (A431 (WT); IC50 of 35 nM).

Western Blot Analysis[1]

Cell Line: CUTO14 (ASV) cells
Concentration: 0.1 nM-1 μM
Incubation Time: 6 h
Result: Robustly inhibited EGFR signaling, reaching 80% and 100% inhibition of phosphorylated EGFR (pEGFR) at concentrations of 100 nM and 1 μM, respectively.

Western Blot Analysis[1]

Cell Line: HCC827 (D), HCC4011 (L), H1975 (LT) cells
Concentration: 0.3 nM-1 μM
Incubation Time: 6 h
Result: Potently inhibited EGFR and downstream signaling in HCC827 (D), HCC4011 (L) and H1975 (LT) cells.

Western Blot Analysis[2]

Cell Line: H1781 (HER2 Exon 20G776>VC), Ba/F3 (HER2 exon 20YVMA) cells
Concentration: 0.01, 0.1 and 1 μM
Incubation Time: 6 h
Result: Inhibited HER2 signaling in H1781 and Ba/F3-HER2 exon 20YVMA mutant cells at 0.1 μM with significantly decreased phosphorylations of HER2, AKT, and ERK1/2 in a dose-dependent manner.
In Vivo

Mobocertinib succinate (3, 10, 30 mg/kg; p.o.; once daily for 20 days) significantly induces tumor growth inhibition[1].

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

Animal Model: Female Athymic Nude-Foxn1nu mice (human NSCLC H1975 LT tumor model)[1].
Dosage: 3, 10, 30 mg/kg
Administration: Oral; once daily for 20 days.
Result: Decreased the mean tumor volume by 44% and 92% when at 3 mg/kg and 10 mg/kg, respectively, relative to the tumor size of vehicle group.
Induced a 76% tumor regression relative to the pretreatment tumor size at 30 mg/kg.
Clinical Trial
Molecular Weight

703.78

Formula

C36H45N7O8

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=CN=C(NC2=CC(NC(C=C)=O)=C(N(CCN(C)C)C)C=C2OC)N=C1C3=CN(C)C4=C3C=CC=C4)OC(C)C.O=C(O)CCC(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (177.61 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4209 mL 7.1045 mL 14.2090 mL
5 mM 0.2842 mL 1.4209 mL 2.8418 mL
10 mM 0.1421 mL 0.7104 mL 1.4209 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (2.96 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (2.96 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.61%

References
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Mobocertinib succinate Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Mobocertinib succinate
Cat. No.:
HY-135815A
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