SM1-71-R
Based on 1 Customer Validation
SM1-71-R is a reversible analog o SM1-71 (HY-136848). SM1-71-R lacks the acrylamide warhead and therefore cannot form a covalent bond with the kinase. SM1-71-R can be used as a control compound for SM1-71.
For research use only. We do not sell to patients.
- Purity : 98.7%
- CAS No.: 2088180-03-2
- Formula: C24H28ClN7O
- Molecular Weight:465.98
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| ASPC1 | IC50 |
73 nM
Compound: 9
|
Antiproliferative activity against human AsPC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human AsPC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay
|
[PMID: 28038940] |
| BaF3 | IC50 |
5 nM
Compound: 9
|
Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay
|
[PMID: 28038940] |
| BaF3 | IC50 |
8 nM
Compound: 9
|
Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay
|
[PMID: 28038940] |
| BaF3 | IC50 |
9 nM
Compound: 9
|
Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs in presence of IL-3 by CellTiter-Glo assay
Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs in presence of IL-3 by CellTiter-Glo assay
|
[PMID: 28038940] |
| PANC-1 | IC50 |
426 nM
Compound: 9
|
Antiproliferative activity against human PANC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human PANC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay
|
[PMID: 28038940] |
| SK-CO-1 | IC50 |
54 nM
Compound: 9
|
Antiproliferative activity against human SKCO1 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human SKCO1 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay
|
[PMID: 28038940] |
| SW-620 | IC50 |
247 nM
Compound: 9
|
Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay
|
[PMID: 28038940] |
In Vitro
SM1-71-R (1 μM; 2 h) results in inhibition of phosphorylation of p-AKTS473 in H23-KRASG12C cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:H23-KRASG12C cells
-
Concentration:1 μM
-
Incubation Time:2 h
-
Result:Resulted in inhibition of phosphorylation of only p-AKTS473, did not inhibit phosphorylation on p-ERK1/2T202/Y204 and p-MEK1/2S217/S221 levels.
Chemical Information
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CAS No. 2088180-03-2
-
Appearance Solid
-
Molecular Weight 465.98
-
Formula C24H28ClN7O
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SMILES
O=C(CC)NC1=C(C=CC=C1)NC2=NC(NC3=CC=C(N(CC4)CCN4C)C=C3)=NC=C2Cl
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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 : 36 mg/mL (77.26 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (269 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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 | 2.1460 mL | 10.7301 mL | 21.4601 mL | 53.6504 mL |
| 5 mM | 0.4292 mL | 2.1460 mL | 4.2920 mL | 10.7301 mL | |
| 10 mM | 0.2146 mL | 1.0730 mL | 2.1460 mL | 5.3650 mL | |
| 15 mM | 0.1431 mL | 0.7153 mL | 1.4307 mL | 3.5767 mL | |
| 20 mM | 0.1073 mL | 0.5365 mL | 1.0730 mL | 2.6825 mL | |
| 25 mM | 0.0858 mL | 0.4292 mL | 0.8584 mL | 2.1460 mL | |
| 30 mM | 0.0715 mL | 0.3577 mL | 0.7153 mL | 1.7883 mL | |
| 40 mM | 0.0537 mL | 0.2683 mL | 0.5365 mL | 1.3413 mL | |
| 50 mM | 0.0429 mL | 0.2146 mL | 0.4292 mL | 1.0730 mL | |
| 60 mM | 0.0358 mL | 0.1788 mL | 0.3577 mL | 0.8942 mL |