1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. Pirtobrutinib

Pirtobrutinib  (Synonyms: LOXO-305)

Cat. No.: HY-131328 Purity: 99.88% ee.: 99.24%
COA Handling Instructions

Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM.

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

Pirtobrutinib Chemical Structure

Pirtobrutinib Chemical Structure

CAS No. : 2101700-15-4

Size Price Stock Quantity
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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 95 In-stock
Solution
10 mM * 1 mL in DMSO USD 95 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 160 In-stock
25 mg USD 370 In-stock
50 mg USD 560 In-stock
100 mg USD 890 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Pirtobrutinib:

Top Publications Citing Use of Products

2 Publications Citing Use of MCE Pirtobrutinib

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM[1].

In Vitro

Pirtobrutinib potently inhibits both wild-type BTK and BTK C481S-mediated kinase activity with nanomolar potency. Pirtobrutinib inhibits WT BTK (Y223) autophosphorylation with an IC50 of 3.68 nM. Pirtobrutinib inhibits BTK C481S Y223, C481T Y223, and C481R Y223 autophosphorylation with IC50s of 8.45, 7.23, and 11.73 nM, respectively[1].

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

Clinical Trial
Molecular Weight

479.43

Formula

C22H21F4N5O3

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=C(N)N([C@@H](C)C(F)(F)F)N=C1C2=CC=C(CNC(C3=CC(F)=CC=C3OC)=O)C=C2)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (104.29 mM; Need ultrasonic; 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 2.0858 mL 10.4291 mL 20.8581 mL
5 mM 0.4172 mL 2.0858 mL 4.1716 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: 2.75 mg/mL (5.74 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

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

    Solubility: ≥ 2.75 mg/mL (5.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.88% ee.: 99.24%

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 (stored under nitrogen). 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 2.0858 mL 10.4291 mL 20.8581 mL 52.1453 mL
5 mM 0.4172 mL 2.0858 mL 4.1716 mL 10.4291 mL
10 mM 0.2086 mL 1.0429 mL 2.0858 mL 5.2145 mL
15 mM 0.1391 mL 0.6953 mL 1.3905 mL 3.4764 mL
20 mM 0.1043 mL 0.5215 mL 1.0429 mL 2.6073 mL
25 mM 0.0834 mL 0.4172 mL 0.8343 mL 2.0858 mL
30 mM 0.0695 mL 0.3476 mL 0.6953 mL 1.7382 mL
40 mM 0.0521 mL 0.2607 mL 0.5215 mL 1.3036 mL
50 mM 0.0417 mL 0.2086 mL 0.4172 mL 1.0429 mL
60 mM 0.0348 mL 0.1738 mL 0.3476 mL 0.8691 mL
80 mM 0.0261 mL 0.1304 mL 0.2607 mL 0.6518 mL
100 mM 0.0209 mL 0.1043 mL 0.2086 mL 0.5215 mL
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Pirtobrutinib 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.

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Product Name:
Pirtobrutinib
Cat. No.:
HY-131328
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