BI-2852 |
| Katalog-Nr.GC35513 |
BI-2852 ist ein KRAS-Inhibitor fÜr die Switch I/II-Tasche (SI/II-Tasche) durch strukturbasiertes Wirkstoffdesign mit nanomolarer AffinitÄt. BI-2852 unterscheidet sich mechanistisch vom kovalenten KRASG12C-Inhibitor (bindet an die Schalter-II-Tasche) und bindet zehnmal stÄrker an aktives KRASG12Dals an KRASwt(740nM gegenÜber 7,5μM). BI-2852 blockiert GEF-, GAP- und Effektor-Wechselwirkungen mit KRAS, was zu einer Hemmung der nachgeschalteten SignalÜbertragung und einer antiproliferativen Wirkung in mutierten KRAS-Zellen fÜhrt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2375482-51-0
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) because it binds to a different pocket present in both the active and inactive forms of KRAS. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells[1].
BI-2852 (Compound 1) (10 nM-10 µM 2 hours) shows a dose-dependent pERK modulation and antiproliferative effect at EC50s of 5.8 μM and 6.7 μM in soft agar and low serum conditions in NCI-H358 cells[1].
References:
[1]. Kessler D, et al. Drugging an undruggable pocket on KRAS. Proc Natl Acad Sci U S A. 2019 Aug 6; 116(32):15823-15829.
| Cas No. | 2375482-51-0 | SDF | |
| Canonical SMILES | OC(C=C1)=CC([C@@H](C2=C(CNCC3=CC4=C(C=CN4CC5=CN(C)C=N5)C=C3)NC6=CC=CC=C62)N7)=C1C7=O | ||
| Formula | C31H28N6O2 | M.Wt | 516.59 |
| Löslichkeit | DMSO: 55 mg/mL (106.47 mM) | Storage | Store at -20°C |
| 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9358 mL | 9.6789 mL | 19.3577 mL |
| 5 mM | 0.3872 mL | 1.9358 mL | 3.8715 mL |
| 10 mM | 0.1936 mL | 0.9679 mL | 1.9358 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 35 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *