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$0.00 - Yosi Shamay, .et al. Quantitative Self-Assembly Prediction Yields Targeted Nanomedicines, Nat Mater, 2018, Apr; 17(4): 361-368 PMID: 29403054
Biological Activity
TAK-632 is a potent pan-RAF inhibitor with favorable in
vitro activity (BRAF(V600E) IC50, 2.4 nM; BRAF(wt), 8.3 nM; CRAF, 1.4 nM; pMEK (A375) IC50, 12 nM; pMEK (HMVII), 49 nM; V/B ratio.
Targets
| Target | Value |
|---|---|
| C-Raf | IC50: 1.4nM |
| B-Raf | IC50: 8.3nM |
| AuroraB | IC50: 66nM |
| PDGFRβ | IC50: 120nM |
| FGFR3 | IC50: 280nM |
| GSK-3β | IC50: 500nM |
| CDK2 | IC50: 580nM |
| p38α | IC50: 600nM |
| PDGFRα | IC50: 610nM |
| Tie-2 | IC50: 740nM |
| CDK1 | IC50: 790nM |
| Chk1 | IC50: 1.4μM |
| MEK1 | IC50: 3.7μM |
| IKKβ | IC50: 3.7μM |
| PKA | IC50: >10μM |
| PKCθ | IC50: >10μM |
| CK1δ | IC50: >10μM |
| ERK1 | IC50: >10μM |
| EGFR | IC50: >10μM |
| HER2 | IC50: >10μM |
| JNK1 | IC50: >10μM |
| c-Met | IC50: >10μM |
| c-Kit | IC50: >10μM |
| Src | IC50: >10μM |
| IR | IC50: >10μM |
| MEKK1 | IC50: >10μM |
| In vitro (25°C) | DMSO | 99 mg/mL (178.53 mM) | |
| Water | Insoluble | ||
| Ethanol | 2 mg/mL (3.6 mM) | ||
| In vivo | 2% DMSO+98% PEG 300 | 4 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 18.03 mL | 90.17 mL | 180.34 mL |
| 0.5 mM | 3.61 mL | 18.03 mL | 36.07 mL |
| 1 mM | 1.8 mL | 9.02 mL | 18.03 mL |
| 5 mM | 0.36 mL | 1.8 mL | 3.61 mL |
*The above data is based on the productmolecular weight 554.51. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A13323 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 1228591-30-7 |
| Formula | C27H18F4N4O3S |
| M. Wt | 554.51 |
| Purity | >98% |
| Synonyms | TAK 632; TAK632 |
| SMILES | C1CC1C(=O)NC2=NC3=C(S2)C(=C(C=C3)OC4=CC(=C(C=C4)F)NC(=O)CC5=CC(=CC=C5)C(F)(F)F)C#N |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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