Src I1
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $879 | Check With Us |
| 500mg | $1200 | Check With Us |
| 1g | $1800 | Check With Us |
: Cat #: V0093 CAS #: 179248-59-0 Purity ≥ 99%
Description: Src Inhibitor 1 (Src-I1) is a novel, potent and selective dual site inhibitor of Src tyrosine kinases with potential anticancer activity. It acts by competitively binding to both the ATP- and peptide-binding sites (IC50 = 44 nM for Src and 88nM for Lck, respectively). Src is a non-receptor tyrosine kinase that is deregulated in many types of cancer. Thus Src Inhibitor 1 (Src-I1) can be potentially used for cancer treatment.
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| Molecular Weight (MW) | 373.41 |
|---|---|
| Molecular Formula | C22H19N3O3 |
| CAS No. | 179248-59-0 |
| Storage | -20℃ for 3 years in powder formrr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: >6 mg/mLrr |
| Water: N/Arr | |
| Ethanol: N/A | |
| SMILES Code | COC1=CC2=NC=NC(NC3=CC=C(OC4=CC=CC=C4)C=C3)=C2C=C1OC |
| Synonyms | Src I1; SrcI1; Src I-1 |
| Protocol | In Vitro | In vitro activity: Src Inhibitor 1 ( Src-I1) is a novel, potent and selective dual site Src tyrosine kinase inhibitor which binds competitively to both the ATP- and peptide-binding sites with IC50 values of 44 nM for Src and 88nM for Lck. Src-I1, is found to be a potent inhibitor of Src (IC50=0.18 μM), but also inhibited other Src family members, such as Lck, Csk and Yes with similar potency to Src, and RIP2 (IC50=0.026 μM) with even greater potency. In addition, it inhibited CHK2 with similar potency to Src, and Aurora B with slightly lower potency. Kinase Assay: All assays (25.5 μl volume) were carried out robotically at room temperature (21 °C) and were linear with respect to time and enzyme concentration under the conditions used. Assays were performed for 30 min using Multidrop Micro reagent dispensers (Thermo Electron Corporation, Waltham, MA, U.S.A.) in a 96-well format. The concentration of magnesium acetate in the assays was 10 mM and [γ-33P]ATP (800 c.p.m./pmol) was used at 5, 20 or 50 μM as indicated, in order to be at or below the Km for ATP for each enzyme. Protein kinases assayed at 5 μM ATP were: MKK1, ERK1, p38γ MAPK, p38δ MAPK, ERK8, PKBα, PKCζ, PRK2, GSK3β, CK2, MARK3, IKKβ, DYRK3, PIM2, EF2K, PLK1, Aurora C, HIPK2 and PAK4. Protein kinases assayed at 20 μM ATP were: JNK1, JNK2, p38β MAPK, PDK1, SGK1, S6K1, PKA, ROCK2, PKCα, MSK1, MAPKAP-K2, MAPKAP-K3, PRAK, CaMKKα, CaMKKβ, CHK1, CHK2, CDK2, Aurora B, CK1, PIM1, PIM3, NEK7, MST2, HIPK3, PAK5, PAK6, CSK, Yes and FGF-R1. Protein kinases assayed at 50 μM ATP were: Eph-A2 (Ephrin-A2 receptor), ERK2, JNK3, p38α MAPK, RSK1, RSK2, PKBβ, PKD1, MNK1, MNK2, AMPK, CaMK1, smMLCK, PHK, BRSK2, MELK, DYRK1a, DYRK2, NEK2a, NEK6, SRPK1, Src, Lck, IKKϵ and TBK1. Protein kinases assayed at 0.1 mM ATP were RIP2, GAK, c-Raf and B-Raf. |
|---|---|---|
| In Vivo | N/A | |
| Animal model | N/A |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.6780 mL | 13.3901 mL | 26.7802 mL | 53.5604 mL |
| 5mM | 0.5356 mL | 2.6780 mL | 5.3560 mL | 10.7121 mL |
| 10mM | 0.2678 mL | 1.3390 mL | 2.6780 mL | 5.3560 mL |
| 20mM | 0.1339 mL | 0.6695 mL | 1.3390 mL | 2.6780 mL |
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%Tween 80
+
%ddH2O
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
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DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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