Pirtobrutinib (Synonyms: LOXO-305, LY3527727) |
| رقم الكتالوجGC62515 |
Pirtobrutinib (LOXO-305) ، مثبط BTK انتقائي للغاية وغير تساهمي من الجيل التالي ، يمنع طفرات استبدال BTK C481 المتنوعةيتسبب Pirtobrutinib في تراجع أورام سرطان الغدد الليمفاوية المعتمدة على BTK في نماذج طعم أجنبي للفأريعتبر Pirtobrutinib أيضًا أكثر من 300 ضعفًا انتقائيًا لـ BTK مقابل 370 كينازات أخرى تم اختبارها ولا يُظهر أي تثبيط كبير للأهداف غير الكينازية عند 1 ميكرومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2101700-15-4
Sample solution is provided at 25 µL, 10mM.
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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].
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].
[1]. Gomez E B , et al. Loxo-305, a Highly Selective and Non-Covalent Next Generation BTK Inhibitor, Inhibits Diverse BTK C481 Substitution Mutations[J]. Blood, 2019, 134(Supplement_1):4644-4644.
| Cas No. | 2101700-15-4 | SDF | |
| المرادفات | LOXO-305, LY3527727 | ||
| Formula | C22H21F4N5O3 | M.Wt | 479.43 |
| الذوبان | DMSO : 50 mg/mL (104.29 mM; Need ultrasonic) | Storage | 4°C, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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