PF-06463922

Catalog No. A14207

PF-06463922是一种有效的双重ALK/ROS1抑制剂，对ROS1，ALK（WT）和ALK（L1196M）的Ki分别为<0.02 nM，<0.07 nM和0.7 nM。

Technical details

Catalog Num	A14207
M. Wt	406.41
Formula	C21H19FN6O2
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	1454846-35-5
Synonyms	PF 06463922, PF06463922
SMILES	C[C@@H]1C2=C(C=CC(=C2)F)C(=O)N(CC3=NN(C(=C3C4=CC(=C(N=C4)N)O1)C#N)C)C

Biological Activity

PF-06463922是一种有效的双重ALK/ROS1抑制剂，对ROS1，ALK（WT）和ALK（L1196M）的Ki分别为<0.02 nM，<0.07 nM和0.7 nM。

Targets

Target	Value
ROS1	ki: <0.02nM
ROS1	ki: <0.02nM
ALK	ki: <0.07nM
ALK(L1196M)	ki: 0.07nM
LTK(TYK1)	IC50: 2.7nM
FER	IC50: 3.3nM
FES(FPS)	IC50: 6nM
PTK2B(FAK2)	IC50: 14nM
TNK2(ACK)	IC50: 17nM
PTK2(FAK)	IC50: 17nM
NTRK2(TRKB)	IC50: 23nM
NTRK2(TRKB)	ki: 23nM
NTRK1(TRKA)	IC50: 24nM
NTRK3(TRKC)	IC50: 46nM
FRK(PTK5)	IC50: 53nM
EGFR(ErbB1)T790ML858R	IC50: 245nM
IGF1R	IC50: 296nM
STK22B(TSSK2)	IC50: 302nM
EGFR(ErbB1)T790M	IC50: 319nM
DCAMKL2(DCK2)	IC50: 370nM
EPHA1	IC50: 375nM
JAK2	IC50: 529nM

Solubility *

In vitro (25°C)	DMSO	Warmed: 70 mg/mL (172.23 mM)
	Water	Insoluble
	Ethanol	Warmed: 26 mg/mL
In vivo	2% DMSO+30% PEG 300+ddH2O	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	24.61 mL	123.03 mL	246.06 mL
0.5 mM	4.92 mL	24.61 mL	49.21 mL
1 mM	2.46 mL	12.3 mL	24.61 mL
5 mM	0.49 mL	2.46 mL	4.92 mL

*The above data is based on the productmolecular weight 406.41. 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.