2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. 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

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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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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Based on 1 publication(s) in Google Scholar

Other Forms of Pirtobrutinib:

Pirtobrutinib Related Antibodies

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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.

Pirtobrutinib Related Antibodies
Clinical Trial
Molecular Weight

479.43

Appearance

Solid

Formula

C22H21F4N5O3
CAS No.
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)

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
10 mM 0.2086 mL 1.0429 mL 2.0858 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

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

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

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.88% ee.: 99.24%

COA (250 KB) HNMR (200 KB) NP-HPLC (589 KB) LCMS (138 KB)

Handling Instructions (2659 KB)
References
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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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  • Dilution Calculator

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Pirtobrutinib2101700-15-4LOXO-305LOXO305LOXO 305BtkBruton tyrosine kinaseWTmutationsC81SproliferativeautophosphorylationInhibitorinhibitorinhibit

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