TAK788 free base · Synonyms: Mobocertinib | AP32788

Mobocertinib (TAK-788; AP32788) is an investigational TKI with potent, selective preclinical activity against activating EGFR and HER2 mutations…

For research use only. Not for human or veterinary use.

Target EGFR

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

TAK788 structure

CAS No.: 1847461-43-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
2 g	USD 495.00	BP-02352-2g	In stock	Get quote
5 g	USD 935.00	BP-02352-5g	In stock	Get quote
10 g	USD 1,600.00	BP-02352-10g	In stock	Get quote
25 g	Inquire	BP-02352-25g	In stock	Inquire
50 g	Inquire	BP-02352-50g	In stock	Inquire

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Description

Mobocertinib (TAK-788; AP32788) is an investigational TKI with potent, selective preclinical activity against activating EGFR and HER2 mutations, including exon 20 insertions. TAK-788 exhibits antitumor activity in pts with EGFR exon 20 insertions with an AE profile consistent with other EGFR TKIs.

Biological activity

Mobocertinib (TAK-788) is an investigational TKI with potent, selective preclinical activity against activating EGFR and HER2 mutations, including exon 20 insertions. Mobocertinib (TAK-788) inhibits all 14 mutant variants of EGFR (IC50s=2.4-22 nM), and all 6 mutant variants of HER2 (IC50s=2.4-26 nM), more potently than it inhibited WT EGFR (IC50=35 nM). Daily oral dosing of Mobocertinib in mice implanted with a patient-derived tumor containing an EGFR exon 20 activating insertion induced regression of tumors at doses that were well tolerated (30-100 mg/kg).

Identifiers

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
InChIKey: AZSRSNUQCUDCGG-UHFFFAOYSA-N

Specifications

MW (average): 585.6966
Formula: C₃₂H₃₉N₇O₄
CAS No.: 1847461-43-1
Physical state: Solid
Color: Off-white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

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.

[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.

Same target

Search EGFR

Same research area

Search Cancer