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

Mavelertinib  (Synonyms: PF-06747775)

Cat. No.: HY-12972 Purity: 99.21%
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Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC).

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

Mavelertinib Chemical Structure

Mavelertinib Chemical Structure

CAS No. : 1776112-90-3

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10 mM * 1 mL in DMSO
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10 mg USD 430 In-stock
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Based on 1 publication(s) in Google Scholar

Mavelertinib Related Antibodies

Top Publications Citing Use of Products

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

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  • Purity & Documentation

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Description

Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC)[1][2][3][4].

IC50 & Target

IC50: 3 nM (T790M/Del), 4 nM (L858R), 5 nM (Del), 12 nM (T790M/L858R), 307 nM (wild-type)[1]
In Vitro

Mavelertinib exhibits selectivity over wild-type EGFR (IC50=307 nM)[1].
Mavelertinib (10 μM) exhibits less than 50% effect or inhibition against all nonkinase targets[1].
Mavelertinib inhibits the hERG26 current with an IC50 > 100 μM[1].

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

Mavelertinib Related Antibodies
In Vivo

Mavelertinib exhibits low to moderate oral bioavailability (mouse 60%, rat 11%, dog 66%) following oral administration (mouse 1, rat 30, dog 3 mg/kg)[1].
Mavelertinib exhibits short plasma half-lives (mouse 0.56, rat 0.28, dog 1.3 h) due to moderate to high plasma clearance (mouse 53, rat 49, dog 12 mL/min/kg) and low steady-state volume of distribution (mouse 1.48, rat 0.66, dog 0.94 L/kg) following intravenous administration (1 mg/kg to mouse, rat and dog)[1].

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

Animal Model: Female Nu/Nu mice[1]
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: P.o. and i.v. administration
Result: Oral bioavailability (60%), T1/2 (1.48 h).
Clinical Trial
Molecular Weight

415.42

Formula

C18H22FN9O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C=CC(N[C@@H]1CN(C2=NC(NC3=CN(C)N=C3OC)=C4N=CN(C)C4=N2)C[C@H]1F)=O
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 : 47.5 mg/mL (114.34 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4072 mL 12.0360 mL 24.0720 mL
5 mM 0.4814 mL 2.4072 mL 4.8144 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.21%

COA (255 KB) HNMR (279 KB) RP-HPLC (223 KB) LCMS (99 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4072 mL 12.0360 mL 24.0720 mL 60.1801 mL
5 mM 0.4814 mL 2.4072 mL 4.8144 mL 12.0360 mL
10 mM 0.2407 mL 1.2036 mL 2.4072 mL 6.0180 mL
15 mM 0.1605 mL 0.8024 mL 1.6048 mL 4.0120 mL
20 mM 0.1204 mL 0.6018 mL 1.2036 mL 3.0090 mL
25 mM 0.0963 mL 0.4814 mL 0.9629 mL 2.4072 mL
30 mM 0.0802 mL 0.4012 mL 0.8024 mL 2.0060 mL
40 mM 0.0602 mL 0.3009 mL 0.6018 mL 1.5045 mL
50 mM 0.0481 mL 0.2407 mL 0.4814 mL 1.2036 mL
60 mM 0.0401 mL 0.2006 mL 0.4012 mL 1.0030 mL
80 mM 0.0301 mL 0.1505 mL 0.3009 mL 0.7523 mL
100 mM 0.0241 mL 0.1204 mL 0.2407 mL 0.6018 mL
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Mavelertinib Related Classifications

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.

Keywords:

Mavelertinib1776112-90-3PF-06747775PF06747775PF 06747775EGFREpidermal growth factor receptorErbB-1HER1tyrosinekinaseTKIDelL858RdoublemutantsT790M/L858RT790M/Delnon-small-cell lungcancerNSCLCInhibitorinhibitorinhibit

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