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

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

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

Mobocertinib mesylate Chemical Structure

CAS No. : 2389149-85-1

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6 Publications Citing Use of MCE Mobocertinib mesylate

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

HER2

EGFR exon 20 insertion

EGFR (WT)

In Vitro

Mobocertinib mesylate (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC₅₀ of 21 nM^[1].
Mobocertinib mesylate (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 mesylate (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells^[1].
Mobocertinib mesylate (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling^[1].
Mobocertinib mesylate (0.01, 0.1 and 1 μM; 6 h) inhibits HER2 signaling in H1781 (HER2 Exon 20^G776>VC), Ba/F3 (HER2 exon 20^YVMA) 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 20^G776>VC), Ba/F3 (HER2 exon 20^YVMA) cells
Concentration:	0.01, 0.1 and 1 μM
Incubation Time:	6 h
Result:	Inhibited HER2 signaling in H1781 and Ba/F3-HER2 exon 20^YVMA mutant cells at 0.1 μM with significantly decreased phosphorylations of HER2, AKT, and ERK1/2 in a dose-dependent manner.

In Vivo

Mobocertinib mesylate (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:	Animal model: Female Athymic Nude-Foxn1^nu 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

681.80

Formula

C₃₃H₄₃N₇O₇S

CAS No.

2389149-85-1

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=S(O)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Gonzalvez F, et al. Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer. Cancer Discov. 2021 Jul;11(7):1672-1687. [Content Brief]

[2]. Han H, et al. Targeting HER2 Exon 20 Insertion-Mutant Lung Adenocarcinoma with a Novel Tyrosine Kinase Inhibitor Mobocertinib. Cancer Res. 2021 Oct 15;81(20):5311-5324. [Content Brief]

Mobocertinib mesylate 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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