TAK-632

Catalog No. A13323

TAK-632是一种有效的泛RAF抑制剂，具有良好的体外活性（BRAF（V600E）IC50，2.4 nM; BRAF（wt），8.3 nM; CRAF，1.4 nM; pMEK（A375）IC50，12 nM; pMEK（HMVII ），49 nM。

Product Citations

Yosi Shamay, .et al. Quantitative Self-Assembly Prediction Yields Targeted Nanomedicines, Nat Mater, 2018, Apr; 17(4): 361-368 PMID: 29403054

Technical details

Catalog Num	A13323
M. Wt	554.51
Formula	C27H18F4N4O3S
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	1228591-30-7
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

Biological Activity

TAK-632是一种有效的泛RAF抑制剂，具有良好的体外活性（BRAF（V600E）IC50，2.4 nM; BRAF（wt），8.3 nM; CRAF，1.4 nM; pMEK（A375）IC50，12 nM; pMEK（HMVII ），49 nM。

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

Solubility *

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.

Preparing Stock Solutions

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.