2. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Pyrotinib

Pyrotinib  (Synonyms: SHR-1258)

Cat. No.: HY-104065 Purity: 99.80%
COA Handling Instructions

Pyrotinib (SHR-1258) est un double inhibiteur de EGFR/HER2 qui est puissant et sélectif avec des IC50s de 13 et 38 nM, respectivement.

Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.

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

Pyrotinib Chemical Structure

Pyrotinib Chemical Structure

CAS No. : 1269662-73-8

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1 mg USD 228 In-stock
5 mg USD 780 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Pyrotinib:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively[1].

IC50 & Target[1]

EGFR

13 nM (IC50)

HER2

38 nM (IC50)

In Vitro

Pyrotinib has high potency in HER2-dependent cell lines (BT474, SK-OV-3), while showing much weaker inhibition in the HER2 negative cell line (MDA-MB-231). It inhibits BT474 and SK-OV-3Pyrotinib cells with IC50s of 5.1 and 43 nM, respectively. Pyrotinib displays high selectivity as HKI-272 when tested in a panel of different kinases such as KDR, c-Kit, PDGFRβ, c-Src and C-Met (c-Src with an IC50 of 790 nM, and others over 3000 nM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

Pyrotinib has acceptable bioavailability of 20.6%, 43.5% and 13.5% in nude mice, rats and dogs, respectively. Pyrotinib has favorable drug-like physicochemical properties and shows relatively higher oral exposure in human subjects with a much longer half life than that of preclinical animal species such as mouse, rat and dog. The TGI % (tumor growth inhibition) of Pyrotinib on day 21 is 109%, 157%, 159% at the doses of 5 mg/kg, 10 mg/kg, 20 mg/kg respectively. Pyrotinib in SK-OV-3 ovarian xenograft model shows TGI% on day 21 of 2%, 12%, 83% at the doses of 2.5 mg/kg, 5 mg/kg, 10 mg/kg respectively), which further confirms its robust in vivo antitumor efficacy at 10 mg/kg[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

583.08

Appearance

Solid

Formula

C32H31ClN6O3
CAS No.
SMILES

O=C(NC1=C(OCC)C=C2N=CC(C#N)=C(NC3=CC=C(OCC4=NC=CC=C4)C(Cl)=C3)C2=C1)/C=C/[[email protected]@H]5N(C)CCC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (17.15 mM; ultrasonic and adjust pH to 6 with HCl)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7150 mL 8.5752 mL 17.1503 mL
5 mM 0.3430 mL 1.7150 mL 3.4301 mL
10 mM 0.1715 mL 0.8575 mL 1.7150 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation

Purity: 99.80%

COA (249 KB) LCMS (273 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

Cancer cells (A431, SK-BR-3 and NCI-N87) are treated with a series of concentrations of Pyrotinib for 72 hours. Cell proliferation is determined by a sulforhodamine B (SRB) method. The IC50 values are calculated by the data of inhibition rates of serial concentrations of test compounds[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats: Test compounds (include Pyrotinib) are administrated in both intravenous (i.v.) and intragastric (i.g.) for mice to obtain their bioavailability. Plasma samples of nude mice is collected at pre-dose and 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 12, 24 h after the IV administration[1].

Mice: In vivo efficacy studies are performed on BALB/Ca-nude mice (6 to 7 weeks, female) from SLAC. Nude mice are hypodermic inoculated BT-474 human breast cancer cell or SK-OV-3 ovarian cancer cell. After tumor grows to 150-250 mm3, mice are randomly divided into groups and dosed with Pyrotinib (2.5, 5, 10, 20 mg/kg) once daily. The volume of tumors and the weight of the mice are measured and recorded for 2-3 times per week[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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Help & FAQs
  • 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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Keywords:

Pyrotinib1269662-73-8SHR-1258SHR1258SHR 1258EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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