Ba/F3-KIF5B-RET(K5,R12S,V804M)激酶Kinase穩定表達細胞株-BioVector NTCC保藏中心
I. Introduction
Cell Line Name：

BA/F3_KIF5B-RET (V804M)

Gene Synonyms:

kinesin family member 5B ，HEL-S-61, KINH, KNS, KNS1, UKHC；ret proto-oncogene，CDHF12, CDHR16, HSCR1, MEN2A, MEN2B, MTC1, PTC-ELE1, RET

Host Cell:

Ba/F3

Stability: 16 passages
Application:

Anti-proliferation assay and PD assay

Freeze Medium:

90% FBS+10% DMSO

Complete Culture Medium:

RPMI-1640+10%FBS+1 ug/ml puromycin

Mycoplasma Status:

Negative


II.Background
Chromosomal rearrangements involving the gene that encodes the RET tyrosine kinase are known oncogenic drivers in 1% to 2% of patients with non–small cell lung cancer (NSCLC). These RET rearrangements occur with characteristic partners, most commonly KIF5B, but also CCDC6, NCOA, TRIM33, CUX1, KIAA1217, FRMD4A, and KIAA1468. They are typically identified in young patients with adenocarcinoma histology and minimal smoking history. Therapeutic targeting of RET-fusion–driven NSCLCs has taken the form of treatment with broad-spectrum tyrosine kinase inhibitors with anti-RET activity, such as cabozantinib (Cabometyx; Cometriq), vandetanib (Caprelsa), lenvatinib (Lenvima), RXDX-105, and sunitinib (Sutent). Cabozantinib and vandetanib have been the most heavily studied multi-kinase inhibitors (MKIs), with response rates of 20% to 50% in largely pretreated patients with RET-rearranged NSCLC. Sunitinib has been used in fewer patients to date with initial results demonstrating a 22% response rate. RXDX-105 has exhibited uniquely impressive response rates (75%) in patients with non–KIF5B-RET-fusion NSCLC, compared with 0% response in patients with KIF5B-RET-fusion–positive NSCLC. BLU-667 has demonstrated an objective response rate of 50% in patients with RET-fusion positive NSCLC, and LOXO-292 reported a 74% ORR in patients with RET-fusion positive NSCLC. Notably, RXDX-105, BLU- 667, and LOXO-292 have all demonstrated some central nervous system activity in these early phase trials. Future directions of RET inhibition in patients with RET-rearranged NSCLC include additional clinical validation of the next generation RET-selective inhibitors RXDX-105, BLU-667, and LOXO-292 and comparing multikinase inhibitors with RET-selective inhibitors to determine the optimal sequencing of RET-targeted therapies.


III. Representative Data
1. Anti-proliferation assay



Figure 1. Anti-proliferation assay of one reference compounds on the BA/F3_KIF5B-RET (V804M) Stable Cell Line


IV. Thawing

Thawing: Protocol
1. Remove the vial from liquid nitrogen tank and thaw cells quickly in a 37°C water-bath.
2. Just before the cells are completely thawed, decontaminate the outside of the vial with 70% ethanol and transfer the cells to a 15 ml centrifuge tube containing 9 ml of complete growth medium.
3. Pellet cells by centrifugation at 200 x g force for 5 min, and discard the medium.
4. Resuspend the cells in complete growth medium.
5. Add 10 ml of the cell suspension in a 10 cm dish.
6. Add promycin to a concentration of 1 μg/ml the following day.
Kinase細胞株



現代新藥研發的關鍵首先是尋找，確定和制備藥物作用靶點。在500多個已發現的藥物靶點里中，GPCR，Ion Channel，Kinase使用的最為廣泛。




激酶(kinase)是一類從高能供體分子（如ATP）轉移磷酸基團到特定靶分子（底物）的酶；這一過程謂之磷酸化。許多腫瘤的發生是由某些與生長相關的“激酶”發生突變導致異常活化引起的，因而針對這些突變激酶的抑制劑能夠有效抑制這些激酶的活性，從而達到抑制癌細胞增長的目的。
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